Obatoclax Mesylate
Cat. No.：YN250184
CAS No. ：803712-79-0
| 产品名称: | Obatoclax Mesylate |
| CAS No.: | 803712-79-0 |
| Chemical Name: | 2-[2-[(3,5-dimethyl-1H-pyrrol-2-yl)methylene]-3-methoxy-2H-pyrrol-5-yl]-1H-indole, monomethanesulfonate |
| Synonyms: | GX15-070 Mesylate |
| 分子量: | 413.49 |
| 分子式: | C₂₁H₂₃N₃O₄S |
| SMILES: | COC1=CC(C2=CC3=C(C=CC=C3)N2)=N/C1=C\C4=C(C=C(N4)C)C.CS(=O)(O)=O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Obatoclax Mesylate (GX15-070 Mesylate) 是 BH3 模拟物，是泛BCL-2家族蛋白抑制剂，对 BCL-2 的Ki值为 220 nM。Obatoclax Mesylate 诱导自噬 (autophagy) 依赖性细胞死亡，并靶向细胞周期蛋白 D1 进行蛋白酶体降解。Obatoclax Mesylate 具有抗癌和广谱抗寄生虫 (antiparasitic) 活性。 |
| IC50和靶点: | [{name:"Bcl-2:220 nM (Ki)"},{name: "Mcl-1:1-7 μM (Ki)"},{name: "Bcl-xL:1-7 μM (Ki)"},{name: "Bcl-W:1-7 μM (Ki)"},{name: "Bcl-B:1-7 μM (Ki)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Shore, G.C., and Viallet, J.Modulating the Bcl-2 family of apoptosis suppressors for potential therapeutic benefit in cancerHematology Am. Soc. Hematol. Educ. Program,226-230(2005)
Konopleva, M., Watt, J., Contractor, R., et al.Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax)Cancer Res.68(9),3413-3420(2008)
Trudel, S., Li, Z.H., Rauw, J., et al.Preclinical studies of the pan-Bcl inhibitor obatoclax (GX015-070) in multiple myelomaBlood109(12),5430-5438(2007)
Andreu-Fernández, V., Genovés, A., Messeguer, A., et al.BH3-mimetics- and cisplatin-induced cell death proceeds through different pathways depending on the availability of death-related cellular componentsPLoS One8(2),e56881(2013)
