CEP-40783 NEW
| Price | $43 | $73 | $173 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: CEP-40783 | CAS No.: 1437321-24-8 |
| Purity: 99.64% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | CEP-40783 |
| Description | CEP-40783 (RXDX-106) is an effective, specific and orally active AXL/c-Met inhibitor (IC50: 7/12 nM). It also inhibits MER and TYRO3 (IC50: 29/19 nM). |
| In vitro | In AXL-transfected 293 gT cells, CEP-40783 is 27-fold more active compared to the recombinant enzyme (IC50: 0.26 nM). In GTL-16 cells, CEP-40783 also has superior activity against c-Met (IC50: 6 nM). The enhanced inhibitory activity of CEP-40783 in cells is attributed to its extended residence time on both c-Met and AXL, similar with a Type II mechanism. CEP-40783 shows high kinome selectivity against 298 kinases with an S90 of 0.04 (fraction of kinases showing >90% inhibition at 1 μM)[1]. |
| In vivo | CEP-40783 showed dose- and time-dependent inhibition of AXL phosphorylation using NCI-H1299 NSCL xenografts with ～80% target inhibition at 0.3 mg/kg 6 h post dose and complete target inhibition to >90% inhibition at 1 mg/kg between 6-24 h, while a 10 mg/kg po dose resulted in complete AXL inhibition up to 48 h post dosing. In AXL/NIH3T3 xenografts, 0.3 mg/kg po resulted in complete tumor regressions. CEP-40783 was also efficacious in reducing spontaneous lymph node and pulmonary metastatic tumor burden in the MDA-MB-231-luc and 4T1-luc orthotopic breast cancer models, respectively, at 10 and 30 mg/kg po. PK/PD evaluation of the c-Met activity of CEP-40783 (10, 30, 55 mg/kg po qdX5d) showed significant to complete inhibition of c-Met phosphorylation in GTL-16 gastric carcinoma xenografts. Efficacy studies in GTL-16 xenografts demonstrated significant anti-tumor efficacy (tumor stasis and regressions) at 10 and 30 mg/kg po. In EBC-1 NSCL xenografts, administration of CEP-40783 (3, 10 and 30 mg/kg, po qd) resulted in dose-related efficacy, with tumor stasis at 3 mg/kg, tumor regressions and >96% TGI at 10 mg/kg. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : Insoluble Ethanol : 2 mg/mL DMSO : 5.89 mg/mL (10 mM), Sonication is recommended. |
| Keywords | Tyro3 | TAM Receptor | RXDX106 | RXDX 106 | Mer | Inhibitor | inhibit | c-Met/HGFR | CEP-40783 | CEP40783 | Axl |
| Inhibitors Related | UNC2025 | Gilteritinib | Capmatinib 2HCl | (±)-Norcantharidin | L-Ascorbic acid 2-phosphate trisodium | Sitravatinib | Crizotinib | NCT-503 | Cabozantinib S-malate | Capmatinib xHCl | Bacitracin Zinc | Capmatinib |
| Related Compound Libraries | Reprogramming Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Active Compound Library |
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
- Address: 36?Washington?Street, Wellesley?Hills
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