1625677-63-5

Name	EGFR-IN-1
CAS	1625677-63-5
Molecular Formula	C28H30N6O4
MDL Number	MFCD30532637
Molecular Weight	514.58
MOL File	1625677-63-5.mol

Synonyms

EGFR-IN-1 EGFR IN 1,EGFRIN1 2-Propenamide, N-[3-[2-[[4-[2-(dimethylamino)ethoxy]-2-methoxyphenyl]amino]-5-methyl-7-oxopyrido[2,3-d]pyrimidin-8(7H)-yl]phenyl]-

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Chemical Properties

density	1.282±0.06 g/cm3(Predicted)
pka	13.18±0.70(Predicted)

Hazard Information

Uses

EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1].

in vivo

EGFR-IN-1 (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight^[1].
EGFR-IN-1 evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h^[1].

Animal Model:	Female athymic nude mice (H1975 Tumor Xenograft)^[1]
Dosage:	30 mg/kg
Administration:	p.o.; daily for 2 weeks
Result:	Led to significant tumor growth inhibition with no observed loss in body weight.

IC 50

EGFR^L858R/T790M

References

[1] Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92. DOI:10.1021/acsmedchemlett.5b00193

Supplier

cjbscvictory

Telephone13348960310 13348960310

Websitehttps://www.weikeqi-biotech.com/

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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