Description
BMS 599626 dihydrochloride is a potent and selective inhibitor of EGFR and ErbB2 with IC50 values of 22 and 32 nM, respectively . The epidermal growth factor receptor (EGFR) is the cell-surface receptor for epidermal growth factor and plays an important role in tumor invasion and cancer cell proliferation. Receptor tyrosine-protein kinase erbB-2 (ErbB2) is a human epidermal growth factor receptor and plays a critical role in breast cancer. BMS 599626 dihydrochloride is a potent and selective EGFR and ErbB2 inhibitor. BMS-599626 inhibited HER4 with IC50 value of 190 nM. In Sal2, N87 and GEO tumor cells, BMS-599626 inhibited phosphorylation of HER1 and HER2 in a dose-dependent way and inhibited cell proliferation. In AU565 breast cancer cells, BMS-599626 (1μM) inhibited HER1/HER2 heterodimer formation . In tumor cells that forming HER1/HER2 heterodimers, BMS-599626 inhibited heterodimerization . In the L2987 human lung tumors xenograft models, BMS-599626 (60 mg/kg) inhibited and delayed tumor growth in a dose-dependent way .
Product information
Molecular Weight: 603.48
Formula: C27H29Cl2FN8O3
Chemical Name: (E)-N-[(4Z)-4-({1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl}imino)-5-methyl-1H,4H-pyrrolo[2,1-f][1,2,4]triazin-6-yl]{[(3S)-morpholin-3-yl]methoxy}carboximidic acid dihydrochloride
Smiles: Cl.Cl.CC1=C2/C(=N/C3C=C4C=NN(CC5=CC(F)=CC=C5)C4=CC=3)/N=CNN2C=C1/N=C(\O)/OC[C@@H]1COCCN1
InChiKey: SKHKFWSXLCGMNF-IKXQUJFKSA-N
InChi: InChI=1S/C27H27FN8O3.2ClH/c1-17-23(34-27(37)39-15-22-14-38-8-7-29-22)13-36-25(17)26(30-16-32-36)33-21-5-6-24-19(10-21)11-31-35(24)12-18-3-2-4-20(28)9-18;;/h2-6,9-11,13,16,22,29H,7-8,12,14-15H2,1H3,(H,34,37)(H,30,32,33);2*1H/t22-;;/m0../s1
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
Products are for research use only. Not for human use.
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