- Avapritinib
-
- $0.00 / 1g
-
2024-06-30
- CAS:1703793-34-3
- Min. Order: 1g
- Purity: More Than 99%
- Supply Ability: 50kg/Month
- BLU-285
-
- $1.00 / 1g
-
2019-12-25
- CAS:1703793-34-3
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 1000KGS
Related articles - Synthesis of Avapritinib
- The synthesis of Avapritinib occurs in two steps and requires the involvement of the intermediate Avapritinib Amine Salt.
- Dec 28，2023
|
| | BLU-285 Basic information |
| Product Name: | BLU-285 | | Synonyms: | BLU-285;CPD1212;(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;Avapritinib(BLU-285);BLU-285 (Avapritinib);BLU-285;BLU 285;BLU285;CS-2474;BLU-N | | CAS: | 1703793-34-3 | | MF: | C26H27FN10 | | MW: | 498.56 | | EINECS: | | | Product Categories: | API | | Mol File: | 1703793-34-3.mol |  |
| | BLU-285 Chemical Properties |
| 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) | | color | White to light yellow | | CAS DataBase Reference | 1703793-34-3 |
| | BLU-285 Usage And Synthesis |
| 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). 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 |
| | BLU-285 Preparation Products And Raw materials |
|