Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR. It has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | 5 days | $ 142.00 | |
5 mg | 5 days | $ 237.00 |
Description | BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR. It has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively. |
Targets&IC50 | EGFR:5 nM, HER2:20 nM, HER4:60 nM |
In vitro | BMS-690514 inhibits members of the VEGFR family with IC50 values in the range of 25 to 50 nM. BMS-690514 targets several critical signaling pathways: human epidermal growth factor receptor (HER)/ErbB, angiogenesis signaling through VEGFR2, lymphangiogenesis through VEGFR3, respectively. It also shows activity against VEGFR1, Flt-3, and Lck. Permeability of BMS-690514 in Caco-2 cells is in the intermediate range with a moderate potential to be a P-gp substrate[2]. Non–small cell lung tumor cells with exon 19 deletion (HCC4006, HCC827, and PC9) are highly sensitive to BMS-690514, which inhibits their proliferation with IC50 values of 2 to 35 nM. Tumor cell lines with EGFR gene amplification (DiFi, NCI-H2073, A431) are also highly sensitive to inhibition by BMS-690514. Breast and gastric tumor cell lines that have HER2 gene amplification (N87, SNU-216, AU565, BT474, KPL4, and HCC202) are inhibited with IC50 values of 20 to 60 nM[1]. Tumor cell lines that are dependent on HER2 signaling are also found to be highly sensitive to BMS-690514. |
In vivo | BMS-690514 can cross the blood–brain barrier with a brain-to-plasma ratio of 1. BMS-690514 has been shown to be efficacious in a broad spectrum of tumor xenografts. At doses that are efficacious and well tolerated in the animal models, BMS-690514 inhibits tumor cell proliferation and tumor blood flow[1]. The preclinical ADME properties of BMS-690514 suggest good oral bioavailability in humans and metabolism by multiple pathways including oxidation and glucuronidation[2]. The oral bioavailability of BMS-690514 is 78% in mice, 100% in rats, 8% in monkeys, and 29% in dogs. |
Molecular Weight | 368.43 |
Formula | C19H24N6O2 |
CAS No. | 859853-30-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 24 mg/mL (65.14 mM)
You can also refer to dose conversion for different animals. More
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BMS-690514 859853-30-8 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors VEGFR EGFR HER inhibit BMS 690514 ErbB-1 Vascular endothelial growth factor receptor Epidermal growth factor receptor Inhibitor BMS690514 HER1 inhibitor