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Epigenetics
HDAC inhibitor
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Apoptosis related activator
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Autophagy activator
Tubastatin A
僅限科研使用
Tubastatin A
Tubastatin A 是一種有效的，選擇性HDAC6抑制劑，無細胞試驗中IC50為15 nM，選擇性遠高于所有其他同工酶(1000倍)除了HDAC8(57倍)。Tubastatin A 可促進自噬并增加凋亡。
Tubastatin A Chemical Structure
CAS: 1252003-15-8
產(chǎn)品質(zhì)控
批次：
純度：
99.63%
99.63
Tubastatin A相關(guān)產(chǎn)品
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 |
|---|---|---|---|---|---|
| KB | Function assay | 14 uM | 24 hrs | Inhibition of HDAC1 in human KB cells assessed as increase in histone H4 acetylation at 14 uM after 24 hrs by Western blotting analysis | 25899338 |
| KMS-12-BM | Function assay | 15 uM | up to 48 hrs | Inhibition of HDAC6 in human KMS-12-BM cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method | 27541357 |
| MOLM14 | Function assay | 15 uM | up to 48 hrs | Inhibition of HDAC6 in human MOLM14 cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method | 27541357 |
| U937 | Function assay | 2 uM | 18 hrs | Inhibition of HDAC6 in human U937 cells assessed as increase in alpha-tubulin acetylation at Lys-40 residue at 2 uM after 18 hrs by Western blot method | 28337317 |
| HEL | Cell cycle assay | 1 to 5 uM | 48 hrs | Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 1 to 5 uM after 48 hrs propidium iodide staining based flow cytometry | 29940115 |
| HeLa | Function assay | 2 uM | 12 hrs | Inhibition of HDAC6 in human HeLa cells assessed as increase in acetyl-tubulin level at 2 uM after 12 hrs by Western blot analysis | 29533873 |
| HEK293 | Function assay | 10 uM | 24 hrs | Inhibition of HDAC1 in HEK293 cells assessed as increase in histone H3 acetylation at 10 uM after 24 hrs by Western blot method | 28523102 |
| MV4-11 | Function assay | 200 nM | 24 hrs | Inhibition of HDAC6 in human MV4-11 cells assessed as accumulation of acetylated alpha-tubulin at 200 nM after 24 hrs by Western blot analysis | 29738953 |
| HCT116 | Cell cycle assay | 5 uM | 48 hrs | Cell cycle arrest in human HCT116 cells assessed as accumulation at sub-G1 phase at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric method | 28038324 |
| PC12 | Neuroprotective assay | 10 uM | 24 hrs | Neuroprotective activity against H2O2-induced toxicity in rat PC12 cells assessed as cell viability at 10 uM pretreated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by MTT assay relative to control | 30385227 |
| PC12 | Neuroprotective assay | 5 uM | 24 hrs | Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay | 30385227 |
| PC12 | Neuroprotective assay | 10 uM | 24 hrs | Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay | 30385227 |
| PC12 | Neuroprotective assay | 5 to 10 uM | 24 hrs | Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 to 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs coincubated with ebselen by MTT assay | 30385227 |
| PC12 | Antioxidant assay | 5 uM | 24 hrs | Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by DCFH-DA dye-based fluorescence analysis | 30385227 |
| PC12 | Antioxidant assay | 5 uM | 24 hrs | Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs coincubated with ebselen by DCFH-DA dye-based fluore | 30385227 |
| Sf9 | Function assay | 30 mins | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 0.013 μM. | 29549837 | |
| Sf9 | Function assay | 2 hrs | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay, IC50 = 0.0035 μM. | 27541357 | |
| Sf9 | Function assay | 90 mins | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using RHKK(Ac) as substrate after 90 mins by fluorimetric method, IC50 = 0.0137 μM. | 28038324 | |
| Sf9 | Function assay | 2 hrs | Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 0.015 μM. | 23009203 | |
| Sf9 | Function assay | 90 mins | Inhibition of human recombinant N-terminal GST-tagged full length HDAC6 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay, IC50 = 0.0304 μM. | 30092367 | |
| HeLaS3 | Function assay | 15 mins | Inhibition of HDAC6 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 0.031 μM. | 28337317 | |
| insect cells | Function assay | 4 hrs | Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using BATCP as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0349 μM. | 27650925 | |
| SHSY5Y | Function assay | 8 hrs | Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0943 μM. | 27650925 | |
| SHSY5Y | Function assay | 8 hrs | Inhibition of HDAC in human SHSY5Y cells using MAL as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.1221 μM. | 27650925 | |
| Sf9 | Function assay | 4 hrs | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 4 hrs fluorescence assay, IC50 = 0.718 μM. | 29549837 | |
| Sf9 | Function assay | 1 hr | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 1 hr fluorescence assay, IC50 = 0.967 μM. | 29549837 | |
| SHSY5Y | Function assay | 8 hrs | Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 1.1097 μM. | 27650925 | |
| Sf9 | Function assay | 30 mins | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 1.54 μM. | 29549837 | |
| Sf9 | Function assay | 90 mins | Inhibition of human recombinant C-terminal His/FLAG-tagged full length HDAC1 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay, IC50 = 1.91 μM. | 30092367 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2 μM. | 27541357 | |
| Sf9 | Function assay | 30 mins | Inhibition of full length human recombinant C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (95 to 489 residues) expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 2.26 μM. | 29549837 | |
| HeLa | Function assay | 6 hrs | Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay, IC50 = 2.5 μM. | 25454270 | |
| HL60 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. | 29940115 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. | 29940115 | |
| HEL | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. | 29940115 | |
| HeLaS3 | Function assay | 15 mins | Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 2.7 μM. | 28337317 | |
| HeLaS3 | Function assay | 15 mins | Inhibition of HDAC3 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 2.9 μM. | 28337317 | |
| Jurkat | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay, IC50 = 3.38 μM. | 24304348 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 3.7 μM. | 27541357 | |
| HL60 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. | 29940115 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. | 29940115 | |
| HEL | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. | 29940115 | |
| HeLaS3 | Function assay | 15 mins | Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 3.9 μM. | 28337317 | |
| CAL27 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CAL27 cells measured after 72 hrs by MTT assay, IC50 = 4.6 μM. | 28581289 | |
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 8.6 μM. | 27541357 | |
| Sf9 | Function assay | 30 mins | Inhibition of full length human recombinant C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 9.97 μM. | 29549837 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 10.4 μM. | 27541357 | |
| Cal27CisR | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Cal27CisR cells measured after 72 hrs by MTT assay, IC50 = 10.8 μM. | 28581289 | |
| LNCAP | Cytotoxicity assay | 72 hrs | Cytotoxicity against androgen-dependent human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay, IC50 = 10.88 μM. | 24304348 | |
| Cal27CisR | Function assay | 18 hrs | Inhibition of HDAC in human Cal27CisR cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 12.1 μM. | 28581289 | |
| KB | Cytotoxicity assay | 72 hrs | Cytotoxicity against human KB cells after 72 hrs by MTS assay, IC50 = 14.81 μM. | 25899338 | |
| THLE2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human THLE2 cells after 72 hrs by vialight cell proliferation assay, LC50 = 15.1 μM. | 29549837 | |
| CAL27 | Function assay | 18 hrs | Inhibition of HDAC in human CAL27 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 16.1 μM. | 28581289 | |
| Sf9 | Function assay | 2 hrs | Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 16.4 μM. | 23009203 | |
| B16 | Growth inhibition assay | 48 hrs | Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay, GI50 = 40.5 μM. | 23009203 | |
| LNCAP | Function assay | 24 hrs | Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation measured after 24 hrs relative to control | 27717544 | |
| human | Function assay | 24 hrs | Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced AR protein level measured after 24 hrs relative to control | 27717544 | |
| PC12 | Cytoprotective assay | 24 hrs | Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based fluorescence analysis | 30385227 | |
| PC12 | Cytoprotective assay | 24 hrs | Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based inverted fluorescence microscopic analysis | 30385227 | |
| Sf9 | Function assay | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate by fluorescence assay, IC50 = 0.011 μM. | 27541357 | ||
| Sf9 | Function assay | Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 0.015 μM. | 23905680 | ||
| Sf9 | Function assay | Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate, IC50 = 0.854 μM. | 23905680 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50 = 2 μM. | 29945795 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50 = 3.7 μM. | 29945795 | ||
| PC3 | Antiproliferative assay | Antiproliferative activity against human PC3 cells, IC50 = 8.6 μM. | 29945795 | ||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells, IC50 = 10.4 μM. | 29945795 | ||
| Sf9 | Function assay | Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 16.4 μM. | 23905680 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Tubastatin A 是一種有效的，選擇性HDAC6抑制劑，無細胞試驗中IC50為15 nM，選擇性遠高于所有其他同工酶(1000倍)除了HDAC8(57倍)。Tubastatin A 可促進自噬并增加凋亡。 | ||
|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | Tubastatin A選擇性作用于所有同工酶除了HDAC8，對所有亞型不含HDAC8，保持超過1000倍的選擇性，對HDAC8具有約57倍的選擇性。2.5 μM Tubastatin A優(yōu)先誘導α-tubulin 高度乙?；?。10 μM Tubastatin A輕微誘導組蛋白乙?；?。Tubastatin A 5 μM開始對同型半胱氨酸誘導的神經(jīng)元細胞死亡具有保護作用，這種作用具有劑量依賴性，10 μM時，達到完全保護。[1]Tubastatin A (10 μM) 作用于膽管癌細胞系，誘導乙?；摩?tubulin水平增加，和初級纖毛表達的恢復，初級纖毛表達的恢復與下調(diào)Hedgehog (Hh)和MAPK信號通路，以及減少細胞增殖率（平均50％）和浸潤（40％）相關(guān)。[2]Tubastatin A作用于LPS刺激的人類 THP-1巨噬細胞，顯著抑制TNF-α和IL-6，IC50分別為272 nM 和 712 nM。Tubastatin A作用于小鼠Raw 264.7巨噬細胞，抑制一氧化氮（NO）分泌，這種作用具有劑量依賴性，IC50為4.2 μM。[3] | |||
|---|---|---|---|---|
| 激酶實驗 | HDAC酶試驗 | |||
| Tubastatin A在實驗 Buffer(50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA，和 20 μM tris(2-carboxyethyl)phosphine) 中溶解和稀釋到終濃度的6倍。HDAC酶在實驗 Buffer 中稀釋到終濃度的1.5倍，與Tubastatin A預(yù)溫育10分鐘，然后加入底物。 通過滴定曲線測得，用于每種酶的FTS(HDAC1, HDAC2, HDAC3, 和HDAC6) 或 MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, 和 HDAC9)量等于米氏常數(shù)(Km)。使用0.3 μM測序級胰蛋白酶將FTS或MAZ-1675在實驗 Buffer中稀釋到終濃度的6倍。底物/胰蛋白酶混合物加入到酶/化合物混合物中，震蕩實驗板60秒，然后置于SpectraMax M5酶標儀上。賴氨酸側(cè)鏈在肽底物中脫乙?；?，監(jiān)測酶促反應(yīng)的7-amino-4-methoxy-coumarin釋放，監(jiān)測30分鐘，計算反應(yīng)的線性速率。 | ||||
| 細胞實驗 | 細胞系 | 人體膽管癌細胞系HuCCT-1 | ||
| 濃度 | ~10 μM | |||
| 孵育時間 | 21 天 | |||
| 方法 | 細胞生長在軟瓊脂中，測評錨定非依賴性生長。約25,000個細胞懸浮在培養(yǎng)基的0.4％瓊脂中，超過1％瓊脂層在6孔板中。每周加入兩次培養(yǎng)基，溫育21天，拍攝圖片。使用Gel-Pro軟件分析菌落的數(shù)量和尺寸。 |
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| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | EGFR / p-AKT / AKT / p-ERK / ERK |
|
29665050 | |
| Immunofluorescence | α-tubulin / Acetylated tubulin HDAC6 |
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23798680 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Tubastatin A降低體內(nèi)膽管癌的生長。Tubastatin A(10 mg/kg)處理同基因大鼠原位膽管癌模型，誘導低于平均瘤重6倍，降低腫瘤重量與肝臟重量和體重（分別為5和5.6倍）的比值。Tubastatin A 處理腫瘤，與對照組相比，顯著降低PCNA陽性細胞的量(34% vs 65%)。[2]Tubastat A按30 mg/kg劑量腹腔注射給藥弗氏完全佐劑（FCA）誘導的動物炎癥模型，顯著抑制鼠爪體積。Tubastat A(30 mg/kg 腹腔注射)處理膠原誘導型關(guān)節(jié)炎DBA1小鼠的爪子組織，顯著降低臨床評分（?70％），和IL-6表達。[3] | |
|---|---|---|
| 動物實驗 | Animal Models | 攜帶膽管癌移植瘤BDEneu的大鼠 |
| Dosages | 10 mg/kg | |
| Administration | 每天腹腔注射 | |
化學信息&溶解度
| 分子量 | 335.4 | 分子式 | C20H21N3O2 |
| CAS號 | 1252003-15-8 | SDF | Download Tubastatin A SDF |
| Smiles | CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 16.7 mg/mL ( (49.79 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(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:
We are planning to order some tubastatin A but I found out there are two versions of it. One has HCl and one does not. Which one do you recommend for live cell use? Will the HCl containing version significantly change the pH?
回答：
S8049 and S2627 have same molecular structure. The only difference is S2627 containing HCl and has higher solubility in DMSO (74 mg/mL vs. S8049 9 mg/mL). Since they are the same molecule, the biological function should be similar. I would recommend to use S2627 for cell culture study.
問題 2:
What’s the vehicle do you recommend to dissolve the compound for in vivo experiments?
回答：
S8049 Tubastatin A can be dissolved in 2% DMSO/30% PEG 300/PBS at 2.5 mg/mL as a clear solution, and it is also a clear solution in 2% DMSO/ corn oil at 2.5 mg/mL. The drug in 2% DMSO/0.5% Tween 80/PBS is a homogeneous suspension at 2.5 mg/mL at first. After stay for a while, the precipitation goes out at the bottom of the tube.
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