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Cell Cycle
Aurora Kinase inhibitor
-
FLT3 inhibitor
-
Bcr-Abl inhibitor
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Autophagy activator
Tozasertib (VX-680)
僅限科研使用
Tozasertib (VX-680)
別名: MK-0457 中文名稱：陶扎色替
Tozasertib (VX-680)是一種pan-Aurora抑制劑，對Aurora A作用最強，無細胞試驗中Kiapp為0.6 nM，而對Aurora B/Aurora C的作用較弱，對Aurora A選擇性比其他55種激酶高100倍。唯二的例外是 Fms-related tyrosine kinase-3 (FLT-3) 和 BCR-ABL tyrosine kinase，也可被 Tozasertib 抑制，對應的Ki值均為30 nM和30 nM。Tozasertib 可誘導凋亡和自噬。Phase 2。
Tozasertib (VX-680) Chemical Structure
CAS: 639089-54-6
產(chǎn)品質控
批次：
純度：
99.99%
99.99
Tozasertib (VX-680)相關產(chǎn)品
相關信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| HeLa | Function assay | 10 to 1000 nM | 48 hrs | Inhibition of Aurora kinase B in human HeLa cells assessed as delay in mitotic arrest by accumulation of multinucleated cells with 4N/8N DNA content at 10 to 1000 nM after 48 hrs by propidium iodide staining-based FACS flow cytometric analysis | 23808327 |
| HCT116 | Antitumor assay | 50 mg/kg | 5 days | Antitumor activity against human HCT116 cells xenografted in athymic nu/nu mouse assessed as reduction in tumor size at 50 mg/kg, iv qd for 5 days per week for 2 weeks measured twice a week | 23808327 |
| HCT116 | Function assay | 100 nM | 24 hrs | Inhibition of cytokinesis in human HCT116 cells at 100 nM after 24 hrs by propidium iodide/RNase staining-based flow cytometric analysis | 30143423 |
| HCT116 | Function assay | 1 uM | 24 hrs | Inhibition of cytokinesis in human HCT116 cells at 1 uM after 24 hrs by propidium iodide/RNase staining-based flow cytometric analysis | 30143423 |
| HCT116 | Function assay | 1 uM | 3 hrs | Inhibition of Aurora B in human HCT116 cells assessed as reduction in histone H3 phosphorylation at Ser10 residue up to 1 uM after 3 hrs by Western blot analysis | 30143423 |
| HeLa | Cell cycle assay | 5 uM | 12 hrs | Cell cycle arrest in human HeLa cells assessed as decrease in cyclin B1 protein expression at 5 uM after 12 hrs by Western blot analysis | 30502115 |
| HeLa | Cell cycle assay | 5 uM | 12 hrs | Cell cycle arrest in human HeLa cells assessed as decrease in cdc2 protein expression at 5 uM after 12 hrs by Western blot analysis | 30502115 |
| HeLa | Function assay | 5 uM | 12 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells at 5 uM after 12 hrs by Western blot analysis | 30502115 |
| HeLa | Function assay | 5 uM | 12 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells at 5 uM after 12 hrs by Western blot analysis | 30502115 |
| HCT15 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT15 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=1.23μM | 30143423 | |
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=0.45μM | 30143423 | |
| L929sA | Function assay | 24 hrs | Inhibition of Aurk mouse L929sA cells transfected with human Fas assessed as increase in nuclear area after 24 hrs in presence of TNF by Hoechst 33342 staining-based microscopic assay, IC50=1.06μM | 29437386 | |
| L929sA | Function assay | 24 hrs | Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 24 hrs followed by TNF and zVAD.fmk addition measured after 3 hrs by Hoechst 33342/propidium iodide staining-based assay, IC50=1.02μM | 29437386 | |
| L929sA | Function assay | 0.5 hrs | Inhibition of RIPK1 in mouse L929sA cells transfected with human Fas assessed as inhibition in TNF-induced necroptosis pretreated for 0.5 hrs followed by TNF and zVAD.fmk addition measured after 3 hrs by Hoechst 33342/propidium iodide staining-based assay, IC50=0.98μM | 29437386 | |
| L929sA | Function assay | 24 hrs | Inhibition of Aurk mouse L929sA cells transfected with human Fas assessed as reduction in cell growth after 24 hrs in presence of TNF by Hoechst 33342 staining-based microscopic assay, IC50=0.97μM | 29437386 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs by CCK8 assay, IC50=4.32μM | 29358147 | |
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay, IC50=2.93μM | 29358147 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by CCK8 assay, IC50=1.3μM | 29358147 | |
| A431 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A431 cells after 48 hrs by CCK8 assay, IC50=0.24μM | 29358147 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay, IC50=0.127μM | 29358147 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay, IC50=0.079μM | 29358147 | |
| U937 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human U937 cells after 48 hrs by CCK8 assay, IC50=0.036μM | 29358147 | |
| HCT8 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT8 cells after 48 hrs by MTT assay, IC50=44.6μM | 25812967 | |
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50=27.3μM | 25812967 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50=19.4μM | 25812967 | |
| HeLa | Function assay | 12 hrs | Inhibition of Aurora B in human HeLa cells after 12 hrs by ELISA method, IC50=0.453μM | 25812967 | |
| HeLa | Function assay | 12 hrs | Inhibition of Aurora A in human HeLa cells after 12 hrs by ELISA method, IC50=0.261μM | 25812967 | |
| HepG2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, TC50=3.3μM | 24910766 | |
| NCI-N87 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=11.6μM | 24681066 | |
| SKBR3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=9.99μM | 24681066 | |
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=5.81μM | 24681066 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=4.32μM | 24681066 | |
| PANC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=4.13μM | 24681066 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=3.05μM | 24681066 | |
| HeLa | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=2.93μM | 24681066 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=1.3μM | 24681066 | |
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.4μM | 24681066 | |
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.24μM | 24681066 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.127μM | 24681066 | |
| K562 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0791μM | 24681066 | |
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0382μM | 24681066 | |
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.036μM | 24681066 | |
| MOLT4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay, IC50=0.0212μM | 24681066 | |
| HCT116 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HCT116 cells after 96 hrs by MTS assay, EC50=0.12μM | 23808327 | |
| sf9 | Function assay | 15 mins | Inhibition of GST-tagged Aurora kinase A catalytic domain (123 to 401 amino acids) (unknown origin) expressed in sf9 cells using tetra(LRRWSLG) as substrate preincubated for 15 mins prior to substrate addition measured after 90 mins by luminescence assay, IC50=0.02μM | 23808327 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=0.38μM | 22572580 | |
| HCT116 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay, IC50=0.3μM | 22572580 | |
| HCT116 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HCT116 cells assessed as distinct polyploidy phenotype after 72 hrs, Activity=0.03μM | 19143567 | |
| HCT116 | Cytotoxicity assay | 10 to 14 days | Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay, IC50=0.024μM | 19143567 | |
| HCT116 | Function assay | 3 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HCT116 cells up to 1 uM after 3 hrs by Western blot analysis | 30143423 | |
| HCT116 | Function assay | 3 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HCT116 cells up to 1 uM after 3 hrs by Western blot method | 30143423 | |
| HeLa | Function assay | 12 hrs | Inhibition of Aurora A phosphorylation at Thr288 residue in human HeLa cells after 12 hrs by ELISA, IC50=0.013μM | 30502115 | |
| HeLa | Function assay | 12 hrs | Inhibition of Aurora B phosphorylation at Thr232 residue in human HeLa cells after 12 hrs by ELISA, IC50=0.148μM | 30502115 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, GI50=35.8μM | 30502115 | |
| LoVo | Antiproliferative assay | 48 hrs | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay, GI50=45.3μM | 30502115 | |
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, GI50=46.2μM | 30502115 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50=35.8μM | 30728112 | |
| LoVo | Antiproliferative assay | 48 hrs | Antiproliferative activity against human LoVo cells after 48 hrs by MTT assay, IC50=45.3μM | 30728112 | |
| HeLa | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50=46.2μM | 30728112 | |
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| NCI-H358 | Antiproliferative assay | Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant at | 28038940 | ||
| NCI-H23 | Antiproliferative assay | Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant at | 28038940 | ||
| Hela | Function assay | Inhibition of recombinant Aurora A kinase derived from human Hela cells using kemptide as substrate in presence of [c-32P]ATP, Ki=0.002μM | 27884697 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.12μM | 23808327 | ||
| HCT116 | Function assay | Inhibition of Aurora B kinase assessed as reduction in histone H3 phosphorylation in human HCT116 cells, IC50=0.055μM | 21802948 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.028μM | 21802948 | ||
| insect | Function assay | Inhibition of human recombinant His-tagged Aurora A kinase expressed in insect cells, IC50=0.0007μM | 21194953 | ||
| BA/F3 | Function assay | Inhibition of Bcr-Abl T315I mutant autophosphorylation in mouse BA/F3 cells, IC50=5μM | 20604564 | ||
| BA/F3 | Antiproliferative assay | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant, IC50=0.03μM | 20604564 | ||
| HeLa | Function assay | Inhibition of phosphotransferase activity of recombinant aurora A expressed in HeLa cells, Ki=0.002μM | 20573509 | ||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells by MTS assay, IC50=0.12μM | 20550212 | ||
| COLO205 | Antiproliferative assay | Antiproliferative activity against human COLO205 cells by [3H]thymidine uptake assay, IC50=0.019μM | 19447622 | ||
| H29 | Function assay | Inhibition of Aurora B assessed as loss of phospho histone H3 in human H29 cells, IC50=0.74μM | 18630890 | ||
| HCT | Function assay | Inhibition of Aurora B assessed as loss of phospho histone H3 in human HCT cells, IC50=0.31μM | 18630890 | ||
| HCT | Function assay | Inhibition of Aurora A assessed as separation of centrosomes in human HCT cells, IC50=0.31μM | 18630890 | ||
| HCT | Function assay | Inhibition of Aurora A in human HCT cells assessed as loss of autophosphorylation of Aurora A, IC50=0.31μM | 18630890 | ||
| HT29 | Antiproliferative assay | Antiproliferative activity against human HT29 cells, IC50=0.15μM | 18630890 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50=0.053μM | 18630890 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50=0.048μM | 18630890 | ||
| TE-5 | Growth Inhibition Assay | IC50=49.7118 μM | SANGRER | ||
| NCI-H345 | Growth Inhibition Assay | IC50=48.468 μM | SANGRER | ||
| TE-6 | Growth Inhibition Assay | IC50=48.446 μM | SANGRER | ||
| L-363 | Growth Inhibition Assay | IC50=46.881 μM | SANGRER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=46.4612 μM | SANGRER | ||
| LS-513 | Growth Inhibition Assay | IC50=45.9156 μM | SANGRER | ||
| COR-L88 | Growth Inhibition Assay | IC50=45.2778 μM | SANGRER | ||
| DG-75 | Growth Inhibition Assay | IC50=45.1577 μM | SANGRER | ||
| NCI-H1694 | Growth Inhibition Assay | IC50=44.9472 μM | SANGRER | ||
| GI-1 | Growth Inhibition Assay | IC50=42.9192 μM | SANGRER | ||
| BC-1 | Growth Inhibition Assay | IC50=42.6731 μM | SANGRER | ||
| KU812 | Growth Inhibition Assay | IC50=41.507 μM | SANGRER | ||
| GDM-1 | Growth Inhibition Assay | IC50=38.9116 μM | SANGRER | ||
| JAR | Growth Inhibition Assay | IC50=38.2449 μM | SANGRER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=38.1654 μM | SANGRER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=37.815 μM | SANGRER | ||
| ES3 | Growth Inhibition Assay | IC50=36.675 μM | SANGRER | ||
| HCC2157 | Growth Inhibition Assay | IC50=35.4619 μM | SANGRER | ||
| TE-441-T | Growth Inhibition Assay | IC50=34.6371 μM | SANGRER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=34.5456 μM | SANGRER | ||
| A253 | Growth Inhibition Assay | IC50=33.5852 μM | SANGRER | ||
| A704 | Growth Inhibition Assay | IC50=33.5538 μM | SANGRER | ||
| COLO-684 | Growth Inhibition Assay | IC50=32.6438 μM | SANGRER | ||
| RXF393 | Growth Inhibition Assay | IC50=32.497 μM | SANGRER | ||
| CHP-126 | Growth Inhibition Assay | IC50=31.1984 μM | SANGRER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=31.1702 μM | SANGRER | ||
| KNS-42 | Growth Inhibition Assay | IC50=30.8956 μM | SANGRER | ||
| Raji | Growth Inhibition Assay | IC50=30.5592 μM | SANGRER | ||
| SW962 | Growth Inhibition Assay | IC50=30.2747 μM | SANGRER | ||
| SNU-C1 | Growth Inhibition Assay | IC50=28.943 μM | SANGRER | ||
| U-266 | Growth Inhibition Assay | IC50=28.6366 μM | SANGRER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=28.6143 μM | SANGRER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=28.0734 μM | SANGRER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=27.5585 μM | SANGRER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=27.1773 μM | SANGRER | ||
| NCI-H748 | Growth Inhibition Assay | IC50=25.7627 μM | SANGRER | ||
| no-11 | Growth Inhibition Assay | IC50=25.747 μM | SANGRER | ||
| MPP-89 | Growth Inhibition Assay | IC50=25.5314 μM | SANGRER | ||
| KP-N-RT-BM-1 | Growth Inhibition Assay | IC50=25.4752 μM | SANGRER | ||
| REH | Growth Inhibition Assay | IC50=25.4671 μM | SANGRER | ||
| NCI-H889 | Growth Inhibition Assay | IC50=25.1931 μM | SANGRER | ||
| LB831-BLC | Growth Inhibition Assay | IC50=25.1526 μM | SANGRER | ||
| KLE | Growth Inhibition Assay | IC50=22.1903 μM | SANGRER | ||
| BOKU | Growth Inhibition Assay | IC50=21.4533 μM | SANGRER | ||
| LP-1 | Growth Inhibition Assay | IC50=21.3432 μM | SANGRER | ||
| EVSA-T | Growth Inhibition Assay | IC50=21.1499 μM | SANGRER | ||
| CAL-148 | Growth Inhibition Assay | IC50=20.9934 μM | SANGRER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=19.8227 μM | SANGRER | ||
| IST-MES1 | Growth Inhibition Assay | IC50=19.6663 μM | SANGRER | ||
| SK-MM-2 | Growth Inhibition Assay | IC50=19.555 μM | SANGRER | ||
| Calu-6 | Growth Inhibition Assay | IC50=19.239 μM | SANGRER | ||
| SF539 | Growth Inhibition Assay | IC50=17.9922 μM | SANGRER | ||
| HH | Growth Inhibition Assay | IC50=17.1963 μM | SANGRER | ||
| ES6 | Growth Inhibition Assay | IC50=16.2361 μM | SANGRER | ||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=15.6326 μM | SANGRER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=14.4433 μM | SANGRER | ||
| NCI-H1417 | Growth Inhibition Assay | IC50=14.3052 μM | SANGRER | ||
| LS-123 | Growth Inhibition Assay | IC50=14.1588 μM | SANGRER | ||
| CTB-1 | Growth Inhibition Assay | IC50=14.0329 μM | SANGRER | ||
| EW-3 | Growth Inhibition Assay | IC50=13.7402 μM | SANGRER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=13.5788 μM | SANGRER | ||
| NEC8 | Growth Inhibition Assay | IC50=13.1038 μM | SANGRER | ||
| HCE-T | Growth Inhibition Assay | IC50=13.0049 μM | SANGRER | ||
| LC4-1 | Growth Inhibition Assay | IC50=12.7706 μM | SANGRER | ||
| KG-1 | Growth Inhibition Assay | IC50=12.6545 μM | SANGRER | ||
| NCI-H1882 | Growth Inhibition Assay | IC50=12.4066 μM | SANGRER | ||
| A3-KAW | Growth Inhibition Assay | IC50=12.3236 μM | SANGRER | ||
| NB1 | Growth Inhibition Assay | IC50=12.29 μM | SANGRER | ||
| OPM-2 | Growth Inhibition Assay | IC50=12.1596 μM | SANGRER | ||
| DMS-153 | Growth Inhibition Assay | IC50=12.0426 μM | SANGRER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=11.9426 μM | SANGRER | ||
| NB69 | Growth Inhibition Assay | IC50=11.7705 μM | SANGRER | ||
| TALL-1 | Growth Inhibition Assay | IC50=11.4058 μM | SANGRER | ||
| LB373-MEL-D | Growth Inhibition Assay | IC50=11.3827 μM | SANGRER | ||
| SJSA-1 | Growth Inhibition Assay | IC50=11.2891 μM | SANGRER | ||
| NCCIT | Growth Inhibition Assay | IC50=11.0582 μM | SANGRER | ||
| SNB75 | Growth Inhibition Assay | IC50=10.076 μM | SANGRER | ||
| KY821 | Growth Inhibition Assay | IC50=9.77484 μM | SANGRER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=9.32844 μM | SANGRER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=8.90265 μM | SANGRER | ||
| KALS-1 | Growth Inhibition Assay | IC50=8.83851 μM | SANGRER | ||
| CP67-MEL | Growth Inhibition Assay | IC50=8.5326 μM | SANGRER | ||
| GCIY | Growth Inhibition Assay | IC50=8.36965 μM | SANGRER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=8.25637 μM | SANGRER | ||
| IA-LM | Growth Inhibition Assay | IC50=7.859 μM | SANGRER | ||
| NCI-H1436 | Growth Inhibition Assay | IC50=7.69932 μM | SANGRER | ||
| KM-H2 | Growth Inhibition Assay | IC50=7.18457 μM | SANGRER | ||
| UACC-257 | Growth Inhibition Assay | IC50=7.04512 μM | SANGRER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=6.78405 μM | SANGRER | ||
| LS-1034 | Growth Inhibition Assay | IC50=6.7566 μM | SANGRER | ||
| DJM-1 | Growth Inhibition Assay | IC50=6.34666 μM | SANGRER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=5.98597 μM | SANGRER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=5.81454 μM | SANGRER | ||
| Daudi | Growth Inhibition Assay | IC50=5.6912 μM | SANGRER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=5.64574 μM | SANGRER | ||
| TE-1 | Growth Inhibition Assay | IC50=5.49004 μM | SANGRER | ||
| TK10 | Growth Inhibition Assay | IC50=5.35469 μM | SANGRER | ||
| MC-CAR | Growth Inhibition Assay | IC50=5.06757 μM | SANGRER | ||
| SF268 | Growth Inhibition Assay | IC50=4.79916 μM | SANGRER | ||
| COR-L279 | Growth Inhibition Assay | IC50=4.75891 μM | SANGRER | ||
| HC-1 | Growth Inhibition Assay | IC50=4.69494 μM | SANGRER | ||
| LU-139 | Growth Inhibition Assay | IC50=4.61835 μM | SANGRER | ||
| TE-12 | Growth Inhibition Assay | IC50=4.56394 μM | SANGRER | ||
| SW872 | Growth Inhibition Assay | IC50=4.3434 μM | SANGRER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=4.22723 μM | SANGRER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=4.02467 μM | SANGRER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=3.9924 μM | SANGRER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=3.95312 μM | SANGRER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=3.94221 μM | SANGRER | ||
| ES1 | Growth Inhibition Assay | IC50=3.92293 μM | SANGRER | ||
| NCI-H2171 | Growth Inhibition Assay | IC50=3.92423 μM | SANGRER | ||
| NOS-1 | Growth Inhibition Assay | IC50=3.84754 μM | SANGRER | ||
| HEL | Growth Inhibition Assay | IC50=3.632 μM | SANGRER | ||
| RPMI-8402 | Growth Inhibition Assay | IC50=3.58603 μM | SANGRER | ||
| PF-382 | Growth Inhibition Assay | IC50=3.35778 μM | SANGRER | ||
| LOUCY | Growth Inhibition Assay | IC50=3.18693 μM | SANGRER | ||
| TE-9 | Growth Inhibition Assay | IC50=3.26736 μM | SANGRER | ||
| RH-1 | Growth Inhibition Assay | IC50=3.17291 μM | SANGRER | ||
| NOMO-1 | Growth Inhibition Assay | IC50=3.02274 μM | SANGRER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=2.91253 μM | SANGRER | ||
| LU-134-A | Growth Inhibition Assay | IC50=2.8926 μM | SANGRER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=2.88126 μM | SANGRER | ||
| SK-N-FI | Growth Inhibition Assay | IC50=2.86868 μM | SANGRER | ||
| NCI-H2107 | Growth Inhibition Assay | IC50=2.83711 μM | SANGRER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=2.83838 μM | SANGRER | ||
| TGW | Growth Inhibition Assay | IC50=2.65832 μM | SANGRER | ||
| ACN | Growth Inhibition Assay | IC50=2.50213 μM | SANGRER | ||
| K5 | Growth Inhibition Assay | IC50=2.40319 μM | SANGRER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=2.4613 μM | SANGRER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=2.29765 μM | SANGRER | ||
| SH-4 | Growth Inhibition Assay | IC50=2.32469 μM | SANGRER | ||
| NB17 | Growth Inhibition Assay | IC50=2.2927 μM | SANGRER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=2.06244 μM | SANGRER | ||
| RPMI-6666 | Growth Inhibition Assay | IC50=2.16207 μM | SANGRER | ||
| ATN-1 | Growth Inhibition Assay | IC50=2.02858 μM | SANGRER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.02654 μM | SANGRER | ||
| SCLC-21H | Growth Inhibition Assay | IC50=1.97057 μM | SANGRER | ||
| GB-1 | Growth Inhibition Assay | IC50=2.01647 μM | SANGRER | ||
| A101D | Growth Inhibition Assay | IC50=1.87395 μM | SANGRER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.83073 μM | SANGRER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=1.78911 μM | SANGRER | ||
| TE-8 | Growth Inhibition Assay | IC50=1.80368 μM | SANGRER | ||
| NCI-H1963 | Growth Inhibition Assay | IC50=1.70583 μM | SANGRER | ||
| NB5 | Growth Inhibition Assay | IC50=1.64229 μM | SANGRER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=1.35405 μM | SANGRER | ||
| CMK | Growth Inhibition Assay | IC50=1.42117 μM | SANGRER | ||
| GT3TKB | Growth Inhibition Assay | IC50=1.28057 μM | SANGRER | ||
| DEL | Growth Inhibition Assay | IC50=1.25643 μM | SANGRER | ||
| SK-LMS-1 | Growth Inhibition Assay | IC50=1.22212 μM | SANGRER | ||
| EW-1 | Growth Inhibition Assay | IC50=1.18562 μM | SANGRER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=1.21111 μM | SANGRER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=1.18005 μM | SANGRER | ||
| HAL-01 | Growth Inhibition Assay | IC50=1.16709 μM | SANGRER | ||
| ETK-1 | Growth Inhibition Assay | IC50=1.13613 μM | SANGRER | ||
| TE-10 | Growth Inhibition Assay | IC50=1.12946 μM | SANGRER | ||
| SBC-1 | Growth Inhibition Assay | IC50=1.12542 μM | SANGRER | ||
| HL-60 | Growth Inhibition Assay | IC50=1.06574 μM | SANGRER | ||
| NKM-1 | Growth Inhibition Assay | IC50=1.02775 μM | SANGRER | ||
| HCC1187 | Growth Inhibition Assay | IC50=1.00505 μM | SANGRER | ||
| DU-4475 | Growth Inhibition Assay | IC50=1.01756 μM | SANGRER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=0.96189 μM | SANGRER | ||
| SF126 | Growth Inhibition Assay | IC50=0.94819 μM | SANGRER | ||
| ES4 | Growth Inhibition Assay | IC50=0.91128 μM | SANGRER | ||
| ML-2 | Growth Inhibition Assay | IC50=0.90259 μM | SANGRER | ||
| ALL-PO | Growth Inhibition Assay | IC50=0.88175 μM | SANGRER | ||
| KGN | Growth Inhibition Assay | IC50=0.89995 μM | SANGRER | ||
| HCE-4 | Growth Inhibition Assay | IC50=0.88063 μM | SANGRER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=0.86385 μM | SANGRER | ||
| HOP-62 | Growth Inhibition Assay | IC50=0.86329 μM | SANGRER | ||
| TE-15 | Growth Inhibition Assay | IC50=0.85098 μM | SANGRER | ||
| HCC1599 | Growth Inhibition Assay | IC50=0.80874 μM | SANGRER | ||
| MC116 | Growth Inhibition Assay | IC50=0.85011 μM | SANGRER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=0.7914 μM | SANGRER | ||
| NB6 | Growth Inhibition Assay | IC50=0.77254 μM | SANGRER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=0.71982 μM | SANGRER | ||
| CCRF-CEM | Growth Inhibition Assay | IC50=0.65346 μM | SANGRER | ||
| ONS-76 | Growth Inhibition Assay | IC50=0.66458 μM | SANGRER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=0.64403 μM | SANGRER | ||
| NCI-H187 | Growth Inhibition Assay | IC50=0.6413 μM | SANGRER | ||
| HT-144 | Growth Inhibition Assay | IC50=0.63798 μM | SANGRER | ||
| CTV-1 | Growth Inhibition Assay | IC50=0.58773 μM | SANGRER | ||
| NCI-SNU-16 | Growth Inhibition Assay | IC50=0.63571 μM | SANGRER | ||
| LS-411N | Growth Inhibition Assay | IC50=0.57752 μM | SANGRER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=0.54392 μM | SANGRER | ||
| KE-37 | Growth Inhibition Assay | IC50=0.52102 μM | SANGRER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=0.43823 μM | SANGRER | ||
| NCI-H524 | Growth Inhibition Assay | IC50=0.51147 μM | SANGRER | ||
| K-562 | Growth Inhibition Assay | IC50=0.43472 μM | SANGRER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=0.42676 μM | SANGRER | ||
| RL95-2 | Growth Inhibition Assay | IC50=0.40567 μM | SANGRER | ||
| BL-70 | Growth Inhibition Assay | IC50=0.38974 μM | SANGRER | ||
| LXF-289 | Growth Inhibition Assay | IC50=0.40406 μM | SANGRER | ||
| MRK-nu-1 | Growth Inhibition Assay | IC50=0.3813 μM | SANGRER | ||
| KARPAS-422 | Growth Inhibition Assay | IC50=0.37272 μM | SANGRER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=0.35178 μM | SANGRER | ||
| IMR-5 | Growth Inhibition Assay | IC50=0.3554 μM | SANGRER | ||
| A388 | Growth Inhibition Assay | IC50=0.34086 μM | SANGRER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=0.33781 μM | SANGRER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.33459 μM | SANGRER | ||
| RKO | Growth Inhibition Assay | IC50=0.30813 μM | SANGRER | ||
| CESS | Growth Inhibition Assay | IC50=0.31328 μM | SANGRER | ||
| NB13 | Growth Inhibition Assay | IC50=0.27984 μM | SANGRER | ||
| EM-2 | Growth Inhibition Assay | IC50=0.26641 μM | SANGRER | ||
| MEG-01 | Growth Inhibition Assay | IC50=0.27849 μM | SANGRER | ||
| SR | Growth Inhibition Assay | IC50=0.24564 μM | SANGRER | ||
| KM12 | Growth Inhibition Assay | IC50=0.2636 μM | SANGRER | ||
| EW-16 | Growth Inhibition Assay | IC50=0.23768 μM | SANGRER | ||
| KS-1 | Growth Inhibition Assay | IC50=0.23785 μM | SANGRER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=0.23337 μM | SANGRER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=0.22591 μM | SANGRER | ||
| ST486 | Growth Inhibition Assay | IC50=0.23087 μM | SANGRER | ||
| PSN1 | Growth Inhibition Assay | IC50=0.22026 μM | SANGRER | ||
| LB647-SCLC | Growth Inhibition Assay | IC50=0.21523 μM | SANGRER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=0.20086 μM | SANGRER | ||
| SW982 | Growth Inhibition Assay | IC50=0.2138 μM | SANGRER | ||
| K052 | Growth Inhibition Assay | IC50=0.1948 μM | SANGRER | ||
| OCUB-M | Growth Inhibition Assay | IC50=0.16983 μM | SANGRER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=0.15965 μM | SANGRER | ||
| SIG-M5 | Growth Inhibition Assay | IC50=0.16707 μM | SANGRER | ||
| TE-11 | Growth Inhibition Assay | IC50=0.14982 μM | SANGRER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.12641 μM | SANGRER | ||
| SW954 | Growth Inhibition Assay | IC50=0.12229 μM | SANGRER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=0.11563 μM | SANGRER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=0.08789 μM | SANGRER | ||
| BL-41 | Growth Inhibition Assay | IC50=0.10445 μM | SANGRER | ||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=0.07879 μM | SANGRER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=0.07782 μM | SANGRER | ||
| ES8 | Growth Inhibition Assay | IC50=0.04613 μM | SANGRER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=0.05299 μM | SANGRER | ||
| NALM-6 | Growth Inhibition Assay | IC50=0.02552 μM | SANGRER | ||
| 697 | Growth Inhibition Assay | IC50=0.02471 μM | SANGRER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=0.01434 μM | SANGRER | ||
| MFH-ino | Growth Inhibition Assay | IC50=0.0099 μM | SANGRER | ||
| BE-13 | Growth Inhibition Assay | IC50=0.00338 μM | SANGRER | ||
| RS4-11 | Growth Inhibition Assay | IC50=0.00404 μM | SANGRER | ||
| Sf9 | Function assay | Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate, IC50=0.023μM | 30234987 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Tozasertib (VX-680)是一種pan-Aurora抑制劑，對Aurora A作用最強，無細胞試驗中Kiapp為0.6 nM，而對Aurora B/Aurora C的作用較弱，對Aurora A選擇性比其他55種激酶高100倍。唯二的例外是 Fms-related tyrosine kinase-3 (FLT-3) 和 BCR-ABL tyrosine kinase，也可被 Tozasertib 抑制，對應的Ki值均為30 nM和30 nM。Tozasertib 可誘導凋亡和自噬。Phase 2。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 雖然VX-680具有多激酶特性，VX-680卻誘導相似的細胞毒性，IC50約為300 nM，在G2/M期，核內復制期，及轉染ABL或FLT-3激酶的BaF3細胞凋亡時，顯示一個Aurora B 類似的抑制表現(xiàn)型。VX-680抑制CAL-62細胞增殖，這種作用存在時間依賴性。用VX-680處理14天，明顯降低群體的數(shù)量和大小，處理8305C下降達到70%，處理CAL-62, 8505C,和BHT-101下降達到90%。用VX-680處理不同ATC細胞，抑制細胞增殖，IC50為25到150 ?nM，這種作用存在時間和劑量依賴性。在軟瓊脂中，VX-680明顯削弱不同細胞系形成群落的能力。caspase-3的活性分析顯示VX-680誘導不同細胞凋亡。VX-680處理CAL-62 細胞12小時，形成DNA含量≥4N細胞累積物。微速攝影分析顯示VX-680處理的CAL-62細胞離開細胞中期。VX-680可以抑制組蛋白H3的磷酸化作用。[2] VX-680作用于攜帶T315I突變的BCR-Abl的病人樣本，具有明顯抑制活性。[3] | |||
|---|---|---|---|---|
| 激酶實驗 | 激酶抑制實驗 | |||
| 丙酮酸激酶/乳酸脫氫酶催化NADH的氧化，伴隨著ATP的消耗，觀察340 nm 處吸光值的降低。反應包括100 mM Tris (pH 為 8), 10 mM MgCl2, 2.2 mM ATP, 1 mM磷酸烯醇丙酮酸, 0.6 mg/ml NADH, 75 ml丙酮酸激酶, 105 ml 乳酸脫氫酶,和0.5 mM 基底肽(序列為EAIYAAPFAKKK)。加入足夠的激酶開始反應，反應的激酶濃度達到30 nM，用微量滴定板分光光度計在30oC進行30分鐘，觀察吸收率的降低。通過加入3.75 μl 溶于100% DMSO的VX-680 或單獨DMSO，獲得抑制常數(shù)。按如下公式計算Ki值，Ki = IC50/(1+[S]/Kd),[S]=[ATP]=2.2 mM, Kd=70 μM。假定作用于野生型和H396P Abl 激酶域的Kd(ATP)為70 μM，計算以上各值。 | ||||
| 細胞實驗 | 細胞系 | CAL-62細胞 | ||
| 濃度 | 5-500 nM | |||
| 孵育時間 | 4天 | |||
| 方法 | 對照組CAL-62細胞培養(yǎng)在二甲亞砜和DMSO中，實驗組加入500?nM VX-680，處理1到5天。加入不同濃度(5到500?nM) Aurora抑制劑處理不同ATC細胞4天，用來測定VX-680作用于細胞增殖的劑量依賴性。細胞在溫育結束前加30?mM BrdU標記，脈沖2小時。通過比色免疫分析使用細胞增殖ELISA試劑盒分析BrdU的合并率。通過比較VX-680處理的細胞和對照組細胞得到結果， |
|||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | DLK / p-MKK7 / MKK7 / p-JNK / JNK p-AURKA / AURKA / Survivin YAP p-AKT / p-GSK3β / Cleaved caspase-3 / Cleaved PARP |
|
23431148 | |
| Immunofluorescence | α-tubulin / Aurora-A |
|
21600017 | |
| Growth inhibition assay | Cell viability |
|
21600017 | |
| 體內研究(In Vivo) | ||
| 體內研究活性 | VX-680作用于人類AML(HL-60)移植瘤模型明顯降低腫瘤尺寸。VX-680按75 mg/kg劑量給藥實驗鼠,每天腹腔注射兩次，持續(xù)13天,與對照組相比，平均腫瘤體積下降達98%。腫瘤體積比實驗之前初始體積小很多。按12.5 mg/kg劑量每天給藥兩次，腫瘤生長也明顯降低，這種作用存在劑量依賴性。VX-680耐受性很好，只有在使用高劑量時可以觀察到實驗動物體重稍微降低。通過比較cisplatin,按5.4 mg/kg劑量給藥，每四天腹腔注射一次，一共進行三次，抑制腫瘤生長只達9%。VX-680作用于胰臟和結腸移植瘤，也引起腫瘤衰退。VX-680靜脈注射給藥攜帶HCT116腫瘤的實驗鼠，顯示很強的抗癌活性。使用高劑量VX-680(每小時2 mg/kg)處理，明顯提高效果，比實驗錢的初始腫瘤平均尺寸下降56%。[1] | |
|---|---|---|
| 動物實驗 | Animal Models | 右側腋窩處皮下注射107 HL-60白血病細胞的雌性無胸腺NCr-nu鼠 |
| Dosages | 50 mg/kg, 75 mg/kg | |
| Administration | 腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00290550 | Terminated | Carcinoma Non-Small-Cell Lung |
Merck Sharp & Dohme LLC |
June 2006 | Phase 2 |
| NCT00111683 | Completed | Chronic Myelogenous Leukemia in Blast Crisis|Lymphocytic Leukemia B Cell Acute|Myelodysplastic Syndromes|Myelogenous Leukemia Chronic |
Merck Sharp & Dohme LLC |
June 2005 | Phase 1 |
化學信息&溶解度
| 分子量 | 464.59 | 分子式 | C23H28N8OS |
| CAS號 | 639089-54-6 | SDF | Download Tozasertib (VX-680) SDF |
| Smiles | CC1=CC(=NN1)NC2=CC(=NC(=N2)SC3=CC=C(C=C3)NC(=O)C4CC4)N5CCN(CC5)C | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 93 mg/mL ( (200.17 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內配方計算器 | ||||
實驗計算
動物體內配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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