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1643497-70-4

1643497-70-4 Structure

1643497-70-4 Structure
IdentificationBack Directory
[Name]

EGFR-IN-2
[CAS]

1643497-70-4
[Synonyms]

EGFR-IN-2
EGFRIN2,EGFR IN 2
[Molecular Formula]

C26H33N9O3S
[MDL Number]

MFCD30747852
[MOL File]

1643497-70-4.mol
[Molecular Weight]

551.67
Chemical PropertiesBack Directory
[Boiling point ]

729.7±70.0 °C(Predicted)
[density ]

1.53±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[pka]

14.95±0.29(Predicted)
Hazard InformationBack Directory
[Description]

EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

EGFR-IN-2 (Compound 21) inhibits EGFR autophosphorylation with IC50s of 0.027 μM, 0.009 μM ,0.033 μM , and 0.218 μM in double mutant TMLR cell line H1975, double mutant TMdel cell line PC9-ER, activating mutant del70% when tested at 0.1 μM, 61-fold over the TMLR Ki and 63-fold over the TMdel Ki)[1].

To examine its inhibitory effect on pEGFR levels in vivo, EGFR-IN-2 (Compound 21) is studied in a mouse H1975 (TMLR) xenograft model. After a single oral dose of 21 at 50 mg/kg, free plasma concentrations of EGFR-IN-2 at or exceeding the in vitro p-EGFR IC50 of 0.027 μM are sustained over 8 h. When administered at 100 mg/kg, the coverage of p-EGFR IC50 is extended to the last measured time point of 16 h postdose. Corresponding knockdown of p-EGFR and the downstream effectors pERK1/2 and AKT levels are observed at those time points, suggesting target engagement in vivo. In mouse, after intravenous and oral administration, the plasma clearance of EGFR-IN-2 is determined to be 104 mL/kg per min with a bioavailability of 19%. In dogs, the plasma clearance is 13 mL/kg per min with an oral bioavailability of 30%[1].

[Uses]

EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
[in vivo]

To examine its inhibitory effect on pEGFR levels in vivo, EGFR-IN-2 (Compound 21) is studied in a mouse H1975 (TMLR) xenograft model. After a single oral dose of 21 at 50 mg/kg, free plasma concentrations of EGFR-IN-2 at or exceeding the in vitro p-EGFR IC50 of 0.027 μM are sustained over 8 h. When administered at 100 mg/kg, the coverage of p-EGFR IC50 is extended to the last measured time point of 16 h postdose. Corresponding knockdown of p-EGFR and the downstream effectors pERK1/2 and AKT levels are observed at those time points, suggesting target engagement in vivo. In mouse, after intravenous and oral administration, the plasma clearance of EGFR-IN-2 is determined to be 104 mL/kg per min with a bioavailability of 19%. In dogs, the plasma clearance is 13 mL/kg per min with an oral bioavailability of 30%[1].

[storage]

Store at -20°C
[References]

[1]. Chan BK, et al. Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor. J Med Chem. 2016 Oct 13;59(19):9080-9093.

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