Asciminib (ABL001) | ABL1 inhibitor | Probechem Biochemicals

Chemical Structure : Asciminib

CAS No.: 1492952-76-7

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Asciminib (ABL-001, ABL001)

货号: PC-62147Not For Human Use, Lab Use Only.

Asciminib (ABL001) is a potent and selective allosteric ABL1 inhibitor with IC50 of 0.25 nM in BCR-ABL1-transformed BaF3 cells.

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5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg	￥3280	In stock
100 mg		Get quote

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生物&药学活性

Asciminib (ABL001) is a potent and selective allosteric ABL1 inhibitor with IC50 of 0.25 nM in BCR-ABL1-transformed BaF3 cells.
Asciminib (ABL-001) binds (Kd=0.5-0.8 nM) to the myristoyl pocket of ABL1 and induces the formation of an inactive kinase conformation.
Asciminib (ABL-001) inhibits phosphorylation of both STAT5 (Tyr694; pSTAT5) and BCR–ABL1 (Tyr245; pBCR–ABL1), and shows selective activity against all BCR–ABL1 cell lines (IC50=1-20 nM).
Asciminib (ABL-001) retains activity against mutated ABL-1 Thr315Ile at low nanomolar concentrations.
Asciminib (ABL-001) is active in vivo, moderate oral absorption.

物理化学性质&存储条件

分子量	449.843
分子式	C20H18ClF2N5O3
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	(R)-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1H-pyrazol-5-yl)nicotinamide

参考文献

1. Wylie AA, et al. Nature. 2017 Mar 30;543(7647):733-737.

2. Lee BJ, et al. Leukemia. 2017 May;31(5):1096-1107.

Asciminib (ABL-001, ABL001)

生物&药学活性

物理化学性质&存储条件

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Asciminib (ABL-001, ABL001)

生物&药学活性

物理化学性质&存储条件

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