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
- MDL Number:
- MFCD31544325
- MOL File:
- 1703793-34-3.mol
| 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 |
| NCI Dictionary of Cancer Terms | avapritinib |
| FDA UNII | 513P80B4YJ |
| NCI Drug Dictionary | avapritinib |
| ATC code | L01EX18 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS07,GHS08 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| 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 price More Price(19)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 22985 | BLU-285 ≥98% | 1703793-34-3 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 22985 | BLU-285 ≥98% | 1703793-34-3 | 5mg | $161 | 2024-03-01 | Buy |
| Cayman Chemical | 22985 | BLU-285 ≥98% | 1703793-34-3 | 10mg | $283 | 2024-03-01 | Buy |
| Cayman Chemical | 22985 | BLU-285 ≥98% | 1703793-34-3 | 25mg | $618 | 2024-03-01 | Buy |
| ChemScene | CS-7577 | Avapritinib 99.94% | 1703793-34-3 | 25mg | $690 | 2021-12-16 | Buy |
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.
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
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 | admin@nexconn.com | China | 10247 | 58 |
| Accela ChemBio Inc. | (+1)-858-699-3322 | info@accelachem.com | United States | 19965 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Neostar United (Changzhou) Industrial Co., Ltd. | +86-519-519-85557386 | marketing1@neostarunited.com | China | 8348 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Chemia Biotechnology（Shanghai） Co., Ltd | +8613816753574 | info@chemia-pharm.com | CHINA | 311 | 58 |
| Wuhan Nutra Biotechnology Co.,Ltd | +8617786394783 | nutrabiotech@outlook.com | China | 300 | 58 |
| Finetech Industry Limited | +86-27-87465837 +8618971612321 | info@finetechnology-ind.com | China | 9634 | 58 |
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
