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Tolinapant

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Chemical Structure| 1799328-86-1 同义名 : ASTX660
CAS号 : 1799328-86-1
货号 : A108877
分子式 : C30H42FN5O3
纯度 : 99%+
分子量 : 539.685
MDL号 : MFCD31619274
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(194.56 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 An orally bioavailable, non-peptidomimetic antagonist of both X chromosome-linked inhibitor of apoptosis protein (XIAP) and cellular IAP 1 (cIAP1), with potential antineoplastic and pro-apoptotic activities. Upon administration, XIAP/cIAP1 antagonist ASTX660 selectively binds to and inhibits the activity of XIAP and cIAP1. This restores and promotes the induction of apoptotic signaling pathways in cancer cells, and inactivates the nuclear factor-kappa B (NF-kB)-mediated survival pathway. XIAP and cIAP1 are overexpressed by many cancer cell types and suppress apoptosis by inhibiting the activity of certain caspases; they promote both cancer cell survival and chemotherapy resistance.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02503423 Solid Tumors ... 展开 >>Lymphoma 收起 << Phase 1 Phase 2 Recruiting December 2019 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.19mL

9.26mL

1.85mL

0.93mL

18.53mL

3.71mL

1.85mL