BMS-690514 NEW
| Price | $142 | $237 |
| Package | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: BMS-690514 | CAS No.: 859853-30-8 |
| Purity: 99.08% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | BMS-690514 |
| Description | BMS-690514 is a potent, orally active inhibitor of EGFR and VEGFR, with IC50 values of 5 nM for EGFR, 20 nM for HER 2, and 60 nM for HER 4. |
| 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 traverse the blood-brain barrier, evidenced by a brain-to-plasma ratio of 1, and exhibits efficacy against a wide range of tumor xenografts. At doses both efficacious and tolerable in animal models, it effectively inhibits tumor cell proliferation and reduces tumor blood flow. Preclinical absorption, distribution, metabolism, and excretion (ADME) studies indicate BMS-690514 possesses favorable oral bioavailability in humans, undergoing metabolism predominantly through oxidation and glucuronidation. Specifically, its oral bioavailability is reported at 78% in mice, 100% in rats, 8% in monkeys, and 29% in dogs. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 24 mg/mL (65.14 mM) |
| Keywords | inhibit | BMS 690514 | ErbB-1 | Vascular endothelial growth factor receptor | Epidermal growth factor receptor | BMS-690514 | Inhibitor | EGFR | BMS690514 | VEGFR | HER1 |
| Inhibitors Related | Nintedanib | Osimertinib | Sorafenib | Lapatinib | Regorafenib | Erlotinib hydrochloride | Erlotinib | Neratinib | Genistein | Gefitinib | Pazopanib | Axitinib |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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