| Identification | Back Directory | [Name]
(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide | [CAS]
1492952-76-7 | [Synonyms]
ABL-001
Asciminib
EOS-61420
L1F3R18W77
ABL001;ABL-001
UNII-L1F3R18W77
asciminib free base
ABL-001 (ASCIMINIB)
Asciminib
(ABL-001)
ABL-001; AB -001; ABL001; ASCIMINIB; ASCIMINIB FREE BASE;
(R)-N- (4-(CHLORODIFLUOROMETHOXY)PHENYL)- 6-(3- HYDROXYPYRROLIDIN-1- YL)-5- (1H-PYRAZOL- 5-YL)NICOTI
(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide
3-Pyridinecarboxamide, N-[4-(chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxy-1-pyrrolidinyl]-5-(1H-pyrazol-3-yl)- | [Molecular Formula]
C20H18ClF2N5O3 | [MDL Number]
MFCD31560488 | [MOL File]
1492952-76-7.mol | [Molecular Weight]
449.84 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C |
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