BLU-945
- CAS No.
- 2660250-10-0
- Chemical Name:
- BLU-945
- Synonyms
- BLU-945;N-[2-[(3S,4R)-3-fluoro-4-methoxy-1-piperidyl]pyrimidin-4-yl]-5-isopropyl-8-[(2R,3S)-2-methyl-3-(methylsulfonylmethyl)azetidin-1-yl]isoquinolin-3-amine;N-[2-[(3S,4R)-3-Fluoro-4-methoxy-1-piperidyl]-4-pyrimidinyl]-5-isopropyl-8-[(2R,3S)-2-methyl-3-[(methylsulfonyl)methyl]-1-azetidinyl]isoquinolin-3-amine;N-(2-((3S,4R)-3-Fluoro-4-methoxypiperidin-1-yl)pyrimidin-4-yl)-5-isopropyl-8-((2R,3S)-2-methyl-3-((methylsulfonyl)methyl)azetidin-1-yl)isoquinolin-3-amine;3-Isoquinolinamine, N-[2-[(3S,4R)-3-fluoro-4-methoxy-1-piperidinyl]-4-pyrimidinyl]-5-(1-methylethyl)-8-[(2R,3S)-2-methyl-3-[(methylsulfonyl)methyl]-1-azetidinyl]-
- CBNumber:
- CB610776751
- Molecular Formula:
- C28H37FN6O3S
- Molecular Weight:
- 556.7
- MOL File:
- 2660250-10-0.mol
- Modify Date:
- 2024/7/2 8:55:12
| Boiling point | 784.6±70.0 °C(Predicted) |
|---|---|
| Density | 1.32±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| form | Solid |
| pka | 7.87±0.10(Predicted) |
| color | Light yellow to yellow |
| InChIKey | LIMFPAAAIVQRRD-MCEZSBKONA-N |
| SMILES | C(C1=CC=C(N2C[C@H](CS(=O)(=O)C)[C@H]2C)C2C=NC(NC3C=CN=C(N4CC[C@@H](OC)[C@@H](F)C4)N=3)=CC1=2)(C)C |&1:7,13,28,31,r| |
BLU-945 Chemical Properties,Uses,Production
Description
BLU-945 is a potent, highly selective, reversible, and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation, and C797S mutation. BLU-945 can be used for research on lung cancer, including non-small cell lung cancer (NSCLC)[1].
Chemical Properties
IUPAC/Chemical Name: N-(2-((3S,4R)-3-fluoro-4-methoxypiperidin-1-yl)pyrimidin-4-yl)-5-isopropyl-8-((2R,3S)-2-methyl-3-((methylsulfonyl)methyl)azetidin-1-yl)isoquinolin-3-amine.
Side effects
According to clinical studies of BLU-945, common side effects of BLU-945 monotherapy include: rash, diarrhoea, nausea, vomiting, headache, dry skin, onychomycosis, and elevated alanine aminotransferase and aspartate aminotransferase. Common side effects of the combination of BLU-945 and ositinib include: headache, nausea, fatigue, decreased appetite, vomiting, diarrhoea, dry skin, acne-like dermatitis and onychomycosis.
in vitro
BLU-945 has inhibitory activity against the EGFRm/T790M double and EGFRm/T790M/C797Striple mutants with IC50 value range from 1.2-4.4 nM.
BLU-945 (0- 10 mM, 4 h) inhibit EGFR phosphorylation in the EGFR L858R/T790M/C797S, and EGFR ex19del/T790M/C797S mutant cell lines.
References
[1] Y. Elamin. “BLU-945 monotherapy and in combination with osimertinib (OSI) in previously treated patients with advanced EGFR-mutant (EGFRm) NSCLC in the phase 1/2 SYMPHONY study.” Journal of Clinical Oncology (2023).
BLU-945 Preparation Products And Raw materials
Raw materials
Preparation Products
BLU-945 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | China | 4695 | 58 | Inquiry |
| Nanjing Shizhou Biotechnology Co., Ltd | +86-15850508050 +86-15850508050 | China | 323 | 58 | Inquiry |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | China | 3136 | 58 | Inquiry |
| Hebei Miaoyin Technology Co.,Ltd | +86-17367732028 +86-17367732028 | China | 3582 | 58 | Inquiry |
| LEAPCHEM CO., LTD. | +86-852-30606658 | China | 43348 | 58 | Inquiry |
| Aladdin Scientific | +1-+1(833)-552-7181 | United States | 52927 | 58 | Inquiry |
| Taizhou Creating Bio-pharm co., ltd. | +8613586099526 | China | 217 | 58 | Inquiry |
| Hebei Weibang Biotechnology Co., Ltd | +8615350571055 | China | 5251 | 58 | Inquiry |
| Wuhan Jiade Ruifeng New Materials Co., Ltd | 18271874579; 18271874579 | China | 268 | 58 | Inquiry |