ChemicalBook > CAS DataBase List > (R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide
(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide
(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide
- CAS No.1492952-76-7
- Chemical Name:(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide
- CBNumber:CB23133462
- Molecular Formula:C20H18ClF2N5O3
- Formula Weight:449.84
- MOL File:1492952-76-7.mol
(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide Property
- 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
- FDA UNII L1F3R18W77
- NCI Drug Dictionary asciminib
Safety
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H302-H315-H319-H335
- Precautionary statements P261-P305+P351+P338
(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide Chemical Properties,Usage,Production
- 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% -
in vivo
Asciminib is undergoing clinical development testing in patients with CML and Philadelphia chromosome-positive acute lymphoblastic leukaemia. Single doses of 7.5, 15 and 30 mg/kg ABL001, administered to mice bearing KCL- 22 xenografts, inhibits pSTAT5 (Tyr694), which return to baseline at 10, 12 and 16-20h after administration of the dose, respectively. In mice implanted with KCL-22 tumors, the minimum dose of asciminib required for complete regression is 7.5 mg/kg twice a day (BID) or 30 mg/kg once a day (QD), and is tolerated at doses up to 250 mg/kg BID. Similarly, in xenografts derived from patients, treatment with 7.5 and 30 mg/kg asciminib leads to regressions that are maintained during dosing[1].
- target BCR-ABL1
(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide Preparation Products And Raw materials
Raw materials
Preparation Products
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(R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide Spectrum
1492952-76-7, (R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamideRelated Search:
- CCT 244747 6-amino-1,3-dimethyl-4-(4-(trifluoromethyl)phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile 1-[2-CHLORO-6-[[(3-IODOPHENYL)METHYL]AMINO]-9H-PURIN-9-YL]-1-DEOXY-N-METHYL-BETA-D-RIBOFURANURONAMIDE Naquotinib (mesylate) HS-173 BI-9564 BenzaMide, 4-[[2-[3,5-bis(trifluoroMethyl)phenyl]-4,5-bis(4-Methoxyphenyl)-1H-iMidazol-1-yl]Methyl]- 4-Propylphenol
- 高纯化学试剂
- 化学试剂
- 杂质对照品
- 抑制剂
- 医药化学试剂
- 合成有机化合物配体
- 原料药
- 标准品
- 细胞生物学试剂
- C20H18ClF2N5O3
- 阿西米尼—游离态
- 阿西米尼—游离态/1492952-76-7
- 化合物ASCIMINIB,10 MM DMSO 溶液
- 阿思尼布API 游离
- (R)-N-(4-(氯二氟甲氧基)苯基)-6-(3-羟基吡咯-1-基)-5- (1H-吡唑-5-基)吡啶-3-酰胺
- ASCIMINIB(阿西米尼)
- 阿思尼布
- ABL-001; AB -001; ABL001; ASCIMINIB;
- ABL-001高含量原粉品质保障
- ASCIMINIB游离态
- 阿西米尼
- N-[4-(氯二氟甲氧基)苯基]-6-[(3R)-3-羟基-1-吡咯烷基]-5-(1H-吡唑-3-基)-3-吡啶甲酰胺
- 化合物ASCIMINIB
- (R)-N-(4-(氯二氟甲氧基)苯基)-6-(3-羟基吡咯-1-基)-5- (1H-吡唑-5-基)烟酸酰胺
- 变构BCR-ABL抑制剂(ASCIMINIB)
- 1492952-76-7
- Asimini
- N-[4-(Chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxy-1-pyrrolidinyl]-5-(1H-pyrazol-3-yl)-3-pyridinecarboxamide
- Asciminib, 10 mM in DMSO
- (R)-N-(4-(Chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1H-pyrazol-3-yl)nicotinamide
- 2H4,15N]-Asciminib
- Asciminib
- ABL-001 (ASCIMINIB)
- Asciminib (ABL-001)
- 3-Pyridinecarboxamide, N-[4-(chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxy-1-pyrrolidinyl]-5-(1H-pyrazol-3-yl)-
- UNII-L1F3R18W77
- L1F3R18W77
- EOS-61420
- (R)-N- (4-(CHLORODIFLUOROMETHOXY)PHENYL)- 6-(3- HYDROXYPYRROLIDIN-1- YL)-5- (1H-PYRAZOL- 5-YL)NICOTI
- asciminib free base
- ABL-001; AB -001; ABL001; ASCIMINIB; ASCIMINIB FREE BASE;
- ABL001;ABL-001
- ABL-001
- (R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide