| Identification | Back Directory | [Name]
BLU-285 | [CAS]
1703793-34-3 | [Synonyms]
BLU-N
BLU-285
CPD1212
CS-2474
Avapritinib
Avapritinib(BLU-285)
BLU-285 (Avapritinib)
BLU-285;BLU 285;BLU285
Avapritinib/CPD1212/Blu285
(1S)-1-(4-Fluorophenyl)-1-(2-{4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl}-5-pyrimidinyl)ethanamine
(S)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazin-1-yl)pyrimidin-5-yl)ethan-1-amine
(S)-alpha-(4-Fluorophenyl)-alpha-methyl-2-[4-[6-(1-methyl-4-pyrazolyl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl]pyrimidine-5-methanamine
5-Pyrimidinemethanamine, α-(4-fluorophenyl)-α-methyl-2-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl]-, (αS)- | [Molecular Formula]
C26H27FN10 | [MDL Number]
MFCD31544325 | [MOL File]
1703793-34-3.mol | [Molecular Weight]
498.56 |
| Chemical Properties | Back Directory | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:83.11(Max Conc. mg/mL);166.7(Max Conc. mM) | [form ]
A crystalline solid | [pka]
6.96±0.10(Predicted) | [CAS DataBase Reference]
1703793-34-3 |
| Hazard Information | Back Directory | [Description]
BLU-285 is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations (IC50s = 0.27 and 0.24 nM for KITD816V and PDGFRαD842V, respectively).1 It is >150-fold selective for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM. BLU-285 also has activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs; IC50s = <100 nM). It inhibits growth of cancer cell lines containing wild-type and mutant KIT and PDGFRα, demonstrating increased potency in cell lines expressing KIT and PDGFRα with activating loop mutations. BLU-285 (0.3-30 mg/kg) reduces tumor volume in a P815 KITD814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies. | [Uses]
Avapritinib is a medication used for the treatment of tumors due to one specific rare mutation. Avapritinib is a potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor. | [Indications]
Avapritinib is approved for the treatment of adult patients with unresectable or metastatic gastrointestinal mesenchymal stromal tumour (GIST) carrying platelet-derived growth factor receptor A (PDGFRA) exon 18 mutations, including the D842V mutation, as well as adult patients with advanced systemic mastocytosis (ASM). | [Brand name]
Ayvakit | [General Description]
Class: receptor tyrosine kinase;
Treatment: GIST, SM;
Other name: BLU-285;
Elimination half-life = 32–57 h;
Protein binding = 98.8% | [target]
Primary targets: PDGFRA, KIT | [storage]
Store at -20°C |
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