| Identification | Back Directory | [Name]
EGFR-IN-1 | [CAS]
1625677-63-5 | [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]- | [Molecular Formula]
C28H30N6O4 | [MDL Number]
MFCD30532637 | [MOL File]
1625677-63-5.mol | [Molecular Weight]
514.58 |
| Hazard Information | Back Directory | [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.
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| [IC 50]
EGFRL858R/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 |
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cjbscvictory
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13348960310 13348960310 |
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www.weikeqi-biotech.com/ |
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