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Chemical Structure : Asciminib
CAS No.: 1492952-76-7
Catalog No.: 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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|---|---|---|---|
| 10 mg | $98 | In stock | |
| 25 mg | $158 | In stock | |
| 50 mg | $258 | In stock | |
| 100 mg | $398 | In stock | |
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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.
| M.Wt | 449.843 | |
| Formula | C20H18ClF2N5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1H-pyrazol-5-yl)nicotinamide |
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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.
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