Asciminib hydrochloride

SKU: orb1940871

Description

Asciminib (ABL001) hydrochloride binds to the myristoyl pocket of ABL1 and induces the formation of an inactive kinase conformation.Asciminib hydrochloride binds potently (dissociation constant=0.5-0.8 nM) and selectively to the myristoyl pocket of ABL1 and induces the inactive C-terminal helix conformation. Asciminib hydrochloride exhibits the same non-ATP-competitive biochemical kinetics as the BCR–ABL inhibitor GNF-2 but with approximately 100-fold greater potency.Asciminib hydrochloride lacks activity against more than 60 kinases, including SRC, and is similarly inactive against G-protein-coupled receptors, ion channels, nuclear receptors and transporters.

Images & Validation

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Key Properties

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CAS Number	2119669-71-3
MW	486.3
Purity	>98% (HPLC)
Formula	C₂₀H₁₉Cl₂F₂N₅O₃
SMILES	O=C(NC1=CC=C(C=C1)OC(Cl)(F)F)C2=CC(C3=NNC=C3)=C(N=C2)N4C[C@@H](CC4)O.[H]Cl
Target	Bcr-Abl
Solubility	DMSO : 100 mg/mL (205.63 mM; Need ultrasonic);H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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Gene Symbol

Bcr-Abl

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