Product Name :
EGFR-IN-1
Description:
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.
CAS:
1625677-63-5
Molecular Weight:
514.58
Formula:
C28H30N6O4
Chemical Name:
N-{3-[2-({4-[2-(dimethylamino)ethoxy]-2-methoxyphenyl}amino)-5-methyl-7-oxo-7H,8H-pyrido[2,3-d]pyrimidin-8-yl]phenyl}prop-2-enamide
Smiles :
CN(C)CCOC1=CC(OC)=C(C=C1)NC1=NC2=C(C=N1)C(C)=CC(=O)N2C1=CC(=CC=C1)NC(=O)C=C
InChiKey:
RGZXAQQHXALOBL-UHFFFAOYSA-N
InChi :
InChI=1S/C28H30N6O4/c1-6-25(35)30-19-8-7-9-20(15-19)34-26(36)14-18(2)22-17-29-28(32-27(22)34)31-23-11-10-21(16-24(23)37-5)38-13-12-33(3)4/h6-11,14-17H,1,12-13H2,2-5H3,(H,30,35)(H,29,31,32)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Cetirizine} medchemexpress|{Cetirizine} Immunology/Inflammation|{Cetirizine} Biological Activity|{Cetirizine} Data Sheet|{Cetirizine} custom synthesis|{Cetirizine} Epigenetic Reader Domain}
Shelf Life:
≥12 months if stored properly.{{Curcumin} MedChemExpress|{Curcumin} Histone Acetyltransferase|{Curcumin} Purity & Documentation|{Curcumin} References|{Curcumin} custom synthesis|{Curcumin} Cancer}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:24179643
Additional information:
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.|Product information|CAS Number: 1625677-63-5|Molecular Weight: 514.58|Formula: C28H30N6O4|Chemical Name: N-{3-[2-({4-[2-(dimethylamino)ethoxy]-2-methoxyphenyl}amino)-5-methyl-7-oxo-7H,8H-pyrido[2,3-d]pyrimidin-8-yl]phenyl}prop-2-enamide|Smiles: CN(C)CCOC1=CC(OC)=C(C=C1)NC1=NC2=C(C=N1)C(C)=CC(=O)N2C1=CC(=CC=C1)NC(=O)C=C|InChiKey: RGZXAQQHXALOBL-UHFFFAOYSA-N|InChi: InChI=1S/C28H30N6O4/c1-6-25(35)30-19-8-7-9-20(15-19)34-26(36)14-18(2)22-17-29-28(32-27(22)34)31-23-11-10-21(16-24(23)37-5)38-13-12-33(3)4/h6-11,14-17H,1,12-13H2,2-5H3,(H,30,35)(H,29,31,32)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|EGFR-IN-1 (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively. EGFR-IN-1 inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively. EGFR-IN-1 highly selective against a panel of 100 kinases.|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. 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.|Products are for research use only. Not for human use.|