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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-AMXI-5001
AMXI-5001

Chemical Structure : AMXI-5001

CAS No.: 2170491-77-5

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AMXI-5001 (AMXI 5001)

货号: PC-72149Not For Human Use, Lab Use Only.

AMXI-5001 (AMXI 5001) is a novel, highly potent, orally active dual PARP1/2 (IC50 5/0.05 nM) and microtubule polymerization inhibitor, inhibits intracellular PAR formation with IC50 of 7 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AMXI-5001 (AMXI 5001) is a novel, highly potent, orally active dual PARP1/2 (IC50 5/0.05 nM) and microtubule polymerization inhibitor, inhibits intracellular PAR formation with IC50 of 7 nM.
AMXI-5001 binds to the catalytic domain of human PARP1 and is a weak tankyrase inhibitor (800-fold lower than IC50 towards either PARP1 or PARP2 enzymes).
AMXI-5001 inhibited tubulin polymerization in a dose-dependent manner.
AMXI-5001 exhibited selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors.
AMXI-5001 is highly active in both BRCA mutated and wild type cancers.
AMXI-5001 elicited a remarkable In vivo preclinical anti-tumor activity in a BRCA mutated TNBC model induced complete regression of established tumors, including exceedingly large tumors, demonstrated superior anti-tumor effects compared to either single agent (PARP or microtubule) inhibitor or combination with both agents.

物理化学性质&存储条件

分子量 457.465
分子式 C25H20FN5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Carbamic acid, N-[6-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorophenyl]-1H-benzimidazol-2-yl]-, ethyl ester

参考文献

1. Hassan Lemjabbar-Alaoui, et al. Am J Cancer Res. 2020 Aug 1;10(8):2649-2676.

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