CHMFL-EGFR-202
- CAS No.
- 2089381-40-6
- Chemical Name:
- CHMFL-EGFR-202
- Synonyms
- CHMFL-EGFR-202;CHMFLEGFR202,CHMFL EGFR 202;2-Propen-1-one, 1-[(3R)-3-[4-amino-3-[3-chloro-4-(2-pyridinylmethoxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-
- CBNumber:
- CB35540386
- Molecular Formula:
- C25H24ClN7O2
- Molecular Weight:
- 489.96
- MDL Number:
- MFCD32174061
- MOL File:
- 2089381-40-6.mol
CHMFL-EGFR-202 Chemical Properties,Uses,Production
Description
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent "DFG-in-C-helix-out" inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines[1]. EGFRT790M|5.3 nM (IC50)|EGFR|8.3 nM (IC50)|ErbB2|8.1 nM (IC50)|ErbB4|3.2 nM (IC50)|MEK1|161 nM (IC50)|Btk|24.5 nM (IC50)|BLK|8.1 nM (IC50)|BMX|111 nM (IC50)
CHMFL-EGFR-202 potently inhibits EGFR primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M[1].CHMFL-EGFR-202 displays strong binding affinities against wild-type, G719C/S, L858R, L858R/T790M, L861Q, and T790M among EGFR wild-type and mutant kinases[1].CHMFL-EGFR-202 also exhibits strong binding affinities against BLK, BMX, BTK, ERBB2, ERBB4, LOK, MEK1, and MEK5 kinases (percent of control score less than 1% at 1 μM)[1].CHMFL-EGFR-202 trongly inhibits BLK, BTK, ERBB2 and ERBB4 with IC50s of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM, respectively[1].CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases with IC50 of 111.0 nM and 161.0 nM[1].
References
[1]. Wang A, et al. Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode.
CHMFL-EGFR-202 Preparation Products And Raw materials
Raw materials
Preparation Products
CHMFL-EGFR-202 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 10000 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 23963 | 58 |
Nanjing Shizhou Biology Technology Co.,Ltd | 025-85560043 15850508050 | cindy.huang@synzest.com | China | 12007 | 58 |
Supplier | Advantage |
---|---|
TargetMol Chemicals Inc. | 58 |
cjbscvictory | 58 |
TargetMol Chemicals Inc. | 58 |
Nanjing Shizhou Biology Technology Co.,Ltd | 58 |