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CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase with IC50 values of 5.3 nM for drug-resistant mutant EGFR T790M and 8.3 nM for WT EGFR kinases.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $117 | In Stock | |
2 mg | $175 | In Stock | |
5 mg | $268 | In Stock | |
10 mg | $395 | In Stock | |
25 mg | $592 | In Stock | |
50 mg | $828 | In Stock | |
100 mg | $1,130 | In Stock | |
1 mL x 10 mM (in DMSO) | $322 | In Stock |
Description | CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase with IC50 values of 5.3 nM for drug-resistant mutant EGFR T790M and 8.3 nM for WT EGFR kinases. |
Targets&IC50 | ErbB2:8.1 nM, EGFR (T790M):5.3 nM, EGFR:8.3 nM, BLK:8.1 nM, MEK1:161 nM, BTK:24.5 nM, ERB4:3.2 nM, BMX:111 nM |
In vitro | CHMFL-EGFR-202 exhibits ∼10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 potently inhibits EGFR primary mutants (L858R, del19) and drug-resistant mutant L858R/T790M. CHMFL-EGFR-202 displays strong binding affinities against wild-type, L861Q, G719C/S, L858R/T790M, L858R, and T790M among EGFR wild-type and mutant kinases. 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). CHMFL-EGFR-202 strongly inhibits BLK, BTK, ERBB2 and ERBB4 (IC50s: of 8.1 nM, 24.5 nM, 8.1 nM and 3.2 nM). CHMFL-EGFR-202 moderately inhibits BMX and MEK1 kinases (IC50s: 111.0 nM and 161.0 nM)[1]. |
Molecular Weight | 489.96 |
Formula | C25H24ClN7O2 |
Cas No. | 2089381-40-6 |
Smiles | NC1=C2C(=NN(C2=NC=N1)[C@H]3CN(C(C=C)=O)CCC3)C4=CC(Cl)=C(OCC5=CC=CC=N5)C=C4 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (91.84 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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