BLU-945

Product Name: BLU-945
CAS No.: 2660250-10-0
Chemical Name: BLU-945
Synonyms: BLU-945;BLU-945 ，E1176;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;N-{2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl}-8-[(2R,3S)-3-(methanesulfonylmethyl)-2-methylazetidin-1-yl]-5-(propan-2-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]-;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 , BLU-945
CBNumber: CB610776751
Molecular Formula: C28H37FN6O3S
Formula Weight: 556.7
MOL File: 2660250-10-0.mol

More

Less

BLU-945 Property

Boiling point:: 784.6±70.0 °C(Predicted)
Density: 1.32±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: Sparingly soluble: 1-10 mg/ml
Ethanol: Slightly soluble: 0.1-1 mg/ml
form: Solid
pka: 7.87±0.10(Predicted)
color: Light yellow to yellow
InChI: InChI=1/C28H37FN6O3S/c1-17(2)20-6-7-24(35-14-19(18(35)3)16-39(5,36)37)22-13-31-27(12-21(20)22)32-26-8-10-30-28(33-26)34-11-9-25(38-4)23(29)15-34/h6-8,10,12-13,17-19,23,25H,9,11,14-16H2,1-5H3,(H,30,31,32,33)/t18-,19-,23+,25-/s3
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|

More

Less

Hazard and Precautionary Statements (GHS)

More

Less

BLU-945 Chemical Properties,Usage,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).
[2] MEREDITH S. ENO*, THOMAS A. DINEEN Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer[J]. Journal of Medicinal Chemistry, 2022, 65 14: 9662-9677. DOI: 10.1021/acs.jmedchem.2c00704

BLU-945 Preparation Products And Raw materials

Raw materials

Preparation Products

More

Less

BLU-945 Suppliers

China 75 United States 4 Global 79

Chengdu DingDang Pharmaceutical Co., Ltd.

Tel: 028-86040038 13980902949;
Fax: 028-85149890
Email: market@dingdangchem.com
Country: China
ProdList: 1853
Advantage: 55

Changzhou Borl Biotechnology Co.,LTD

Tel: 13606124132;13656121842
Email: luyan0021@163.com
Country: China
ProdList: 235
Advantage: 58

Suzhou Ryan Pharmaceutical Technology Co., Ltd.

Tel: 0512-68780025 18962125825
Email: sales@ryanchem.com
Country: China
ProdList: 167
Advantage: 62

Chunchuang (Wuhan) Technology Co., Ltd

Tel: 15727060112
Email: yutianchun2007@126.com
Country: China
ProdList: 9814
Advantage: 58

Nanjing Chemlin Chemical Co., Ltd

Tel: 025-83697070
Fax: +86-25-83453306
Email: info@chemlin.com.cn
Country: China
ProdList: 16075
Advantage: 64

BOC Sciences

Tel: 1-631-485-4226; 16314854226
Email: info@bocsci.com
Country: United States
ProdList: 12952
Advantage: 65

Shanghai Hope Chem Co., Ltd.，

Tel: +21-18501659228 18501659228
Fax: sales@hope-chem.com
Email: info@hope-chem.com
Country: China
ProdList: 474
Advantage: 55

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3506
Advantage: 58

Shanghai Pansopharm Technology Co., Ltd.

Tel: 021-20962833 15316628753
Fax: 021-2096-2832
Email: sales@pansopharm.com
Country: China
ProdList: 724
Advantage: 60

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4768
Advantage: 55

2660250-10-0, BLU-945Related Search:

BLU 9931 BLU-782 Pralsetinib Avapritinib Disperse Blue 359

BLU-945

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-methoxy-1-piperidyl]pyrimidin-4-yl]-5-isopropyl-8-[(2R,3S)-2-methyl-3-(methylsulfonylmethyl)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]-

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

N-{2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl}-8-[(2R,3S)-3-(methanesulfonylmethyl)-2-methylazetidin-1-yl]-5-(propan-2-yl)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 , BLU-945

BLU-945 ，E1176

2660250-10-0

blu945