(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide Chemical Properties

Boiling point:

631.7±55.0 °C(Predicted)

Density 

1.518±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:93.0(Max Conc. mg/mL);206.74(Max Conc. mM)
Ethanol:90.0(Max Conc. mg/mL);200.07(Max Conc. mM)

form 

A crystalline solid

pka

10.81±0.70(Predicted)

color 

White to off-white

(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide Usage And Synthesis

Description

Asciminib is the first-in-class Specifically Targeting the ABL1 Myristoyl Pocket (STAMP) inhibitor, which was granted accelerated approval in 2021 for patients with Philadelphia chromosomepositive (Ph+) chronic myeloid leukemia (CML) in chronic phase, previously treated with two or more tyrosine kinase inhibitors (TKIs), and for adult patients with Ph+ CML in chronic phase with the T315I mutation. Asciminib binds to a myristoyl site of the BCR-ABL1 protein and locks the protein into an inactive conformation through a mechanism distinct from those of all other orthosteric TKIs such as imatinib, thus overcoming drug resistance arising from ATPbinding site mutations. Asciminib mimics the function of the myristoylated N-terminus of ABL1 and restores the natural autoinhibition of the ABL1b protein.

Uses

Asciminib comprises ABL kinase inhibitors and/or SLC7A11 inhibitors for the treatment of cancer and central nervous system (CNS) disorders.

General Description

Class: non-receptor tyrosine kinase
Treatment: CML
Elimination half-life = 14.2 h
Protein binding = 97%

target

BCR-ABL1

(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide(1492952-76-7)Related Product Information

• CCT 244747
• 6-amino-1,3-dimethyl-4-(4-(trifluoromethyl)phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
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• Naquotinib (mesylate)
• HS-173
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