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CHMFL-EGFR-202

🥰Excellent
Catalog No. T10802Cas No. 2089381-40-6

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.

CHMFL-EGFR-202

CHMFL-EGFR-202

🥰Excellent
Purity: 99.19%
Catalog No. T10802Cas No. 2089381-40-6
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 SizePriceAvailabilityQuantity
1 mg$117In Stock
2 mg$175In Stock
5 mg$268In Stock
10 mg$395In Stock
25 mg$592In Stock
50 mg$828In Stock
100 mg$1,130In Stock
1 mL x 10 mM (in DMSO)$322In Stock
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Purity:99.19%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight489.96
FormulaC25H24ClN7O2
Cas No.2089381-40-6
SmilesNC1=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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.0410 mL10.2049 mL20.4098 mL102.0491 mL
5 mM0.4082 mL2.0410 mL4.0820 mL20.4098 mL
10 mM0.2041 mL1.0205 mL2.0410 mL10.2049 mL
20 mM0.1020 mL0.5102 mL1.0205 mL5.1025 mL
50 mM0.0408 mL0.2041 mL0.4082 mL2.0410 mL

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