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Saracatinib (AZD0530)
中文名稱：塞卡替尼
Saracatinib (AZD0530)是一種有效的Src抑制劑，無細胞試驗中IC50為2.7 nM，對c-Yes， Fyn， Lyn， Blk， Fgr和Lck也具有活性；但對Abl和EGFR (L858R和L861Q)活性較低。Saracatinib可誘導(dǎo)自噬。Phase 2/3。
Saracatinib (AZD0530) Chemical Structure
CAS: 379231-04-6
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Saracatinib (AZD0530)相關(guān)產(chǎn)品
| 相關(guān)靶點 | Lck Fyn Lyn Yes Fgr | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | PP2 SU6656 PP1 WH-4-023 Src Inhibitor 1 RK 24466 Myristic Acid eCF506 Tolimidone (MLR-1023) UM-164 | 點擊展開 |
| 相關(guān)化合物庫 | 酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫 血管生成相關(guān)化合物庫 HIF-1信號通路化合物庫 FDA抗癌藥物庫 | 點擊展開 |
相關(guān)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 |
|---|---|---|---|---|---|
| Huh7 | Antiviral assay | 2.5 uM | 5 days | Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control | 17360676 |
| Huh7 | Antiviral assay | 2.5 uM | 6 days | Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control | 17360676 |
| Vero | Antiviral assay | 2.5 uM | 4 days | Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control | 17360676 |
| Vero | Antiviral assay | 2.5 uM | 6 days | Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control | 17360676 |
| C6/36 | Antiviral assay | 2.5 uM | 4 days | Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control | 17360676 |
| C6/36 | Antiviral assay | 2.5 uM | 5 days | Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control | 17360676 |
| Vero | Antiviral assay | 2.5 uM | 5 days | Inhibition of viral spread in Dengue virus-infected african green monkey Vero cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 5 days by immunofluorescence assay relative to control | 17360676 |
| Huh7 | Antiviral assay | 2.5 uM | 4 days | Inhibition of viral spread in Dengue virus-infected human Huh7 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 4 days by immunofluorescence assay relative to control | 17360676 |
| C6/36 | Antiviral assay | 2.5 uM | 6 days | Inhibition of viral spread in Dengue virus-infected asian tiger mosquito C6/36 cells assessed as accumulation of viral envelope protein within perinuclear region at 2.5 uM after 6 days by immunofluorescence assay relative to control | 17360676 |
| HEK293 | Function assay | 0.1 to 1 uM | 16 hrs | Inhibition of collagen I-induced DDR2 (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting | 26191369 |
| HEK293 | Function assay | 0.1 to 1 uM | 16 hrs | Inhibition of collagen I-induced DDR2 I638F mutant (unknown origin) phosphorylation expressed in HEK293 cells at 0.1 to 1 uM after 16 hrs by Western blotting | 26191369 |
| HEK293 | Function assay | 1 hr | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0398 μM. | 29941193 | |
| HEK293 | Function assay | 1 hr | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.418 μM. | 29941193 | |
| Rh30 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human Rh30 cells after 48 hrs by CellTiter-Glo luminescent assay, IC50 = 10.1 μM. | 23787099 | |
| Vero | Antiviral assay | 3 days | Antiviral activity against Dengue virus infected in african green monkey Vero cells administered after viral challenge after 3 days by viral plaque assay | 17360676 | |
| SH-4 | Growth Inhibition Assay | IC50=4.25259 μM | SANGER | ||
| PF-382 | Growth Inhibition Assay | IC50=3.83698 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=3.73433 μM | SANGER | ||
| KNS-42 | Growth Inhibition Assay | IC50=3.65 μM | SANGER | ||
| LC-2-ad | Growth Inhibition Assay | IC50=3.557 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=3.31174 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=3.20767 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=3.12109 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=3.05299 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=2.87005 μM | SANGER | ||
| IST-SL2 | Growth Inhibition Assay | IC50=2.72379 μM | SANGER | ||
| SNB75 | Growth Inhibition Assay | IC50=2.68594 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=2.57408 μM | SANGER | ||
| BL-70 | Growth Inhibition Assay | IC50=2.47422 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=2.35723 μM | SANGER | ||
| MZ1-PC | Growth Inhibition Assay | IC50=2.29356 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=2.25714 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=2.18507 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=2.17178 μM | SANGER | ||
| GI-1 | Growth Inhibition Assay | IC50=2.16084 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=2.05958 μM | SANGER | ||
| KALS-1 | Growth Inhibition Assay | IC50=1.98722 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=1.92093 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=1.88574 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=1.84688 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=1.79833 μM | SANGER | ||
| MFH-ino | Growth Inhibition Assay | IC50=1.7787 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=1.71782 μM | SANGER | ||
| RL95-2 | Growth Inhibition Assay | IC50=1.66902 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=1.66252 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=1.55453 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=1.55083 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=1.50246 μM | SANGER | ||
| ST486 | Growth Inhibition Assay | IC50=1.45852 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=1.44105 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=1.43418 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=1.37497 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=1.27687 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=1.2436 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=1.20507 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=1.19779 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=0.90669 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=0.8921 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=0.87275 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=0.86203 μM | SANGER | ||
| NCI-H1436 | Growth Inhibition Assay | IC50=0.79049 μM | SANGER | ||
| NCCIT | Growth Inhibition Assay | IC50=0.73218 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.65249 μM | SANGER | ||
| EW-24 | Growth Inhibition Assay | IC50=0.62693 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=0.60529 μM | SANGER | ||
| D-336MG | Growth Inhibition Assay | IC50=0.50304 μM | SANGER | ||
| K-562 | Growth Inhibition Assay | IC50=0.44967 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=0.44196 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=0.3268 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.28116 μM | SANGER | ||
| TE-15 | Growth Inhibition Assay | IC50=0.27412 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=0.265 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=0.23688 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=0.1599 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=0.06143 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=4.32416 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=4.41864 μM | SANGER | ||
| KURAMOCHI | Growth Inhibition Assay | IC50=4.65256 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=4.66416 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=4.81344 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=4.82373 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=5.49684 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=5.61262 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=5.63667 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=6.01811 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=6.02075 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=6.53074 μM | SANGER | ||
| SR | Growth Inhibition Assay | IC50=6.58807 μM | SANGER | ||
| BB49-HNC | Growth Inhibition Assay | IC50=6.73206 μM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=6.78377 μM | SANGER | ||
| HUTU-80 | Growth Inhibition Assay | IC50=6.98466 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=7.82737 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=7.94904 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=8.42808 μM | SANGER | ||
| GDM-1 | Growth Inhibition Assay | IC50=8.97292 μM | SANGER | ||
| LC4-1 | Growth Inhibition Assay | IC50=9.00911 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=9.15006 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=9.30192 μM | SANGER | ||
| BOKU | Growth Inhibition Assay | IC50=9.96466 μM | SANGER | ||
| EVSA-T | Growth Inhibition Assay | IC50=10.6568 μM | SANGER | ||
| D-283MED | Growth Inhibition Assay | IC50=10.9176 μM | SANGER | ||
| NB1 | Growth Inhibition Assay | IC50=11.0242 μM | SANGER | ||
| RPMI-8402 | Growth Inhibition Assay | IC50=11.178 μM | SANGER | ||
| NCI-H1355 | Growth Inhibition Assay | IC50=11.1806 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=11.3297 μM | SANGER | ||
| RPMI-6666 | Growth Inhibition Assay | IC50=12.9567 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=13.2701 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=13.5948 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=13.9234 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=14.3915 μM | SANGER | ||
| SKM-1 | Growth Inhibition Assay | IC50=14.4499 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=14.7591 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=14.7898 μM | SANGER | ||
| ECC4 | Growth Inhibition Assay | IC50=17.0277 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=17.4655 μM | SANGER | ||
| LB647-SCLC | Growth Inhibition Assay | IC50=17.4949 μM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=18.5256 μM | SANGER | ||
| L-540 | Growth Inhibition Assay | IC50=18.8109 μM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=19.51 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=20.0099 μM | SANGER | ||
| MPP-89 | Growth Inhibition Assay | IC50=23.2289 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=23.8658 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=23.9255 μM | SANGER | ||
| EC-GI-10 | Growth Inhibition Assay | IC50=24.5989 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=26.0203 μM | SANGER | ||
| TGBC1TKB | Growth Inhibition Assay | IC50=26.434 μM | SANGER | ||
| Daudi | Growth Inhibition Assay | IC50=27.0773 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=27.081 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=27.488 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=27.9123 μM | SANGER | ||
| COLO-320-HSR | Growth Inhibition Assay | IC50=28.0373 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=28.1287 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=28.7773 μM | SANGER | ||
| LC-1F | Growth Inhibition Assay | IC50=29.7346 μM | SANGER | ||
| SCLC-21H | Growth Inhibition Assay | IC50=30.7317 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=32.5598 μM | SANGER | ||
| D-247MG | Growth Inhibition Assay | IC50=32.9773 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=33.0362 μM | SANGER | ||
| MONO-MAC-6 | Growth Inhibition Assay | IC50=33.5048 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=33.7666 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=33.7928 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=35.144 μM | SANGER | ||
| A253 | Growth Inhibition Assay | IC50=35.7429 μM | SANGER | ||
| HCC1599 | Growth Inhibition Assay | IC50=36.7053 μM | SANGER | ||
| EB-3 | Growth Inhibition Assay | IC50=36.9518 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=37.3224 μM | SANGER | ||
| SW684 | Growth Inhibition Assay | IC50=41.8495 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=42.0522 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=42.1676 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=43.4596 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=44.3925 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=44.5034 μM | SANGER | ||
| RCC10RGB | Growth Inhibition Assay | IC50=44.7392 μM | SANGER | ||
| CP67-MEL | Growth Inhibition Assay | IC50=45.6241 μM | SANGER | ||
| NB17 | Growth Inhibition Assay | IC50=45.6643 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=45.9464 μM | SANGER | ||
| JiyoyeP-2003 | Growth Inhibition Assay | IC50=46.0119 μM | SANGER | ||
| HCE-4 | Growth Inhibition Assay | IC50=46.5968 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=46.7682 μM | SANGER | ||
| KARPAS-422 | Growth Inhibition Assay | IC50=47.0895 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=47.1622 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=47.6828 μM | SANGER | ||
| PSN1 | Growth Inhibition Assay | IC50=47.7813 μM | SANGER | ||
| NIH3T3 | Function assay | Inhibition of human c-Src in NIH3T3 cells, IC50 = 0.0027 μM. | 17064066 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 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 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Saracatinib (AZD0530)是一種有效的Src抑制劑，無細胞試驗中IC50為2.7 nM，對c-Yes， Fyn， Lyn， Blk， Fgr和Lck也具有活性；但對Abl和EGFR (L858R和L861Q)活性較低。Saracatinib可誘導(dǎo)自噬。Phase 2/3。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | Saracatinib是第一個作用于人類腫瘤組織Src通路的抑制劑。 | |||||||||||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Saracatinib也有效抑制其他Src酪氨酸激酶家族成員，包括c-Yes, Fyn, Lyn, Blk, Fgr, 和Lck，IC50為4到10 nM。Saracatinib有效抑制SrcY530F突變的NIH 3T3細胞，IC50為80 nM。在NBT-II膀胱癌細胞中，Saracatinib顯著阻斷HT1080細胞通過立體骨膠原基質(zhì)的入侵，且完全抑制EGF誘導(dǎo)的細胞分散。[1]Saracatinib作用于DU145和PC3細胞，通過抑制Y419磷酸化而有效抑制Src激活。Saracatinib抑制前列腺癌包括PC3, DU145, CWR22Rv1和 LNCaP的生長，而Saracatinib作用于 LAPC-4, PZ-HPV7和RWPE-1細胞時卻顯示低活性。Saracatinib使細胞周期停止在G1/S期，但是不使caspase 3斷裂。Saracatinib 也明顯抑制Boyden 小室的DU145和PC3 移動。[2]Saracatinib有效且持久抑制Akt，且增強A549和Calu-6細胞對放射處理的敏感性。[3]Saracatinib在活性，再吸收，及組成上抑制蝕骨細胞。Saracatinib也可逆阻斷蝕骨細胞前體的移動。[4] |
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|---|---|---|---|---|
| 激酶實驗 | 激酶實驗 | |||
| 使用受體和非受體酪氨酸激酶的重組催化區(qū)，通過酶聯(lián)免疫吸附法測定酪氨酸激酶活性的IC50值。加入的Saracatinib劑量從0.001到10 mM不等。針對絲氨酸/蘇氨酸激酶的特定實驗是加32P 的滲透捕捉實驗。在加入10 μL 20mM Mg.ATP開始反應(yīng)前，包含0.5 μL Saracatinib或DMSO（作對照) 或pH 3.0 buffer（作對照）的多支路384孔板加入15 μL酶和肽/蛋白底物溫育5分鐘。 所有酶的最終濃度都接近米氏常數(shù)（Km）。實驗在室溫下進行30分鐘，然后加入5 μL正磷酸終止反應(yīng)?；旌虾?，孔中的內(nèi)含物加到P81聯(lián)合板上，使用正磷酸作為洗滌緩沖液，然后計算IC50值。 | ||||
| 細胞實驗 | 細胞系 | PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7，和RWPE-1細胞 | ||
| 濃度 | 62.5 nM-16 mM | |||
| 孵育時間 | 1, 3，和5天 | |||
| 方法 | PC3, DU145, CWR22Rv1, LNCaP, LAPC-4, PZ-HPV7 及RWPE-1細胞按2×103密度接種在96孔板上，溫育過夜。加入濃度不等（62.5 nM-16 mM）的Saracatinib。1,3,5天后分離培養(yǎng)基，每孔加入0.2 mL DMSO，按每分鐘200輪持續(xù)震蕩96孔板15分鐘。MTT實驗測IC50值。 |
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| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | pY576-FAK / pY861-FAK / FAK pY418 Src / Src / pY410 CAS / CAS / Py421 Cortactin / Cortactin p-Akt / p-mTOR / Akt / mTOR / p-S6 / S6 / p-AMPKα / AMPKα |
|
20551056 | |
| Growth inhibition assay | Cell number |
|
24349321 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Saracatinib作用于Src3T3異體移植物顯示出強的腫瘤生長抑制率，且Saracatinib造成Calu-6, MDA-MB-231, AsPc-1和BT474C移植瘤生長適當(dāng)延遲。[1]Saracatinib處理常位DU145鼠，按鼠體重，每千克每天口服處理25mg Saracatinib，結(jié)果顯示出強的抗癌活性。[2] |
|
|---|---|---|
| 動物實驗 | Animal Models | 移植DU145細胞的CB17鼠 |
| Dosages | 25 mg/kg | |
| Administration | 每天口服處理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04598919 | Active not recruiting | Idiopathic Pulmonary Fibrosis (IPF) |
National Jewish Health|Yale University|Icahn School of Medicine at Mount Sinai|AstraZeneca|National Center for Advancing Translational Sciences (NCATS)|Baylor University|International Center for Health Outcomes and Innovation Research |
November 12 2020 | Phase 1|Phase 2 |
| NCT04307953 | Recruiting | Fibrodysplasia Ossificans Progressiva |
Amsterdam UMC location VUmc|Royal National Orthopaedic Hospital NHS Trust|Klinikum Garmisch-Patenkirchen|University of Oxford|Brigham and Women''s Hospital|AstraZeneca|Innovative Medicines Initiative |
August 5 2020 | Phase 2 |
| NCT02085603 | Completed | Cancer |
Sheffield Teaching Hospitals NHS Foundation Trust|AstraZeneca |
March 2014 | Phase 2 |
| NCT01864655 | Completed | Alzheimer''s Disease |
Stephen M. Strittmatter|National Institute of Neurological Disorders and Stroke (NINDS)|Yale University |
July 2013 | Phase 1 |
| NCT01000896 | Withdrawn | Cancer|Non Small Cell Lung Cancer|Epithelial Ovarian Cancer |
AstraZeneca |
January 2010 | Phase 1 |
化學(xué)信息&溶解度
| 分子量 | 542.03 | 分子式 | C27H32ClN5O5 |
| CAS號 | 379231-04-6 | SDF | Download Saracatinib (AZD0530) SDF |
| Smiles | CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 100 mg/mL ( (184.49 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 100 mg/mL (184.49 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)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(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)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(nèi)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(jié)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(nèi)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(nèi)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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常見問題及建議解決方法
問題 1:
What is the half-life of Saracatinib?
回答：
Based on the following paper, the half-life of Saracatinib in vivo is around 40hours and it reaches its peak lever around 2-4 hours after dosing: http://clincancerres.aacrjournals.org/content/16/19/4876.long
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