BLU-285
- CAS No.
- 1703793-34-3
- Chemical Name:
- BLU-285
- Synonyms
- Avapritinib;BLU-N;CS-2474;CPD1212;BLU-285;abaprotinib;Avapritinib(BLU-285);13C,2H3]-Avapritinib;BLU-285 (Avapritinib);BLU-285;BLU 285;BLU285
- CBNumber:
- CB13171751
- Molecular Formula:
- C26H27FN10
- Molecular Weight:
- 498.56
- MOL File:
- 1703793-34-3.mol
- Modify Date:
- 2024/7/18 18:48:45
| 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 |
| InChIKey | DWYRIWUZIJHQKQ-JKXWNSIXNA-N |
| SMILES | C1N(C2N=CC([C@@](N)(C3C=CC(F)=CC=3)C)=CN=2)CCN(C2C3=CC(C4C=NN(C)C=4)=CN3N=CN=2)C1 |&1:6,r| |
| CAS DataBase Reference | 1703793-34-3 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS07,GHS08 |
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|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H315-H317-H319-H332-H334-H340-H350-H360-H373-H412 | |||||||||
| Precautionary statements | P201-P202-P264b-P271-P272-P280-P285-P302+P352-P304+P340-P305+P351+P338-P308+P313-P342+P311-P362+P364-P403-P501c | |||||||||
| NFPA 704 |
|
BLU-285 Chemical Properties,Uses,Production
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.
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
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32760 | 60 | Inquiry |
| Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 | China | 10312 | 58 | Inquiry |
| Accela ChemBio Inc. | +1-858699-3322 +86-18019713315 | United States | 19965 | 58 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29826 | 58 | Inquiry |
| Wuhan Nutra Biotechnology Co.,Ltd | +8617786394783 | China | 300 | 58 | Inquiry |
| Finetech Industry Limited | +86-27-87465837 +8618971612321 | China | 9618 | 58 | Inquiry |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
| Beijing Mesochem Technology Co.,Ltd | +8613651027935 | China | 191 | 58 | Inquiry |
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- Dec 28，2023