BMS-794833 |
| Catalog No.GC13833 |
Met/VEGFR-2 inhibitor,potent and ATP-competitive
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1174046-72-0
Sample solution is provided at 25 µL, 10mM.
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BMS-794833 is a potent ATP competitive, dual inhibitor of c-Met and VEGFR2 (IC50 = 1.7 nM and 15 nM, respectively). It also has inhibitory effect on Ron, Axl and Flt3 (IC50 < 3 nM).
c-MET, also called MET, is a membrane receptor that is essential for embryonic development and wound healing. VEGFR are receptors for vascular endothelial growth factor and belong to receptor tyrosine kinases. It mediates in various cellular functions, including endothelial proliferation, migration, survival, tubular morphogenesis and sprouting. [1]
BMS794833 also inhibited gastric cancer cell line (GTL-16) that induced by c-Met receptor, GTL-16, IC50 = 39 Nm [1]. In human gastric tumor xenografts model, BM798433 exhibits > 50% TGI for at least one tumor doubling time without significant toxicity in 14 days. In U87 glioblastoma model, 25mg/kg of BMS798433 exert complete tumor stasis. [1]
Reference:
[1] 4-pyridinone compounds and their use of cancer, Borzilleri et al, United States patent application publication, Pub No. : US 2012/0114643 A1, Pub.Date: May 10, 2012.
Cell experiment: | GTL-16 cells are inoculated in to 96 well microtiter plates in 0.5% fetal calf serum and incubated at 37°C, 5% CO2, 95% air and 100% relative humidity for 24 h prior to addition of a compound. Cells are treated with BMS-794833 for an additional 72 h. Growth inhibition is calculated[1]. |
References: [1]. WO2009094417 | |
| Cas No. | 1174046-72-0 | SDF | |
| Chemical Name | N-[4-(2-amino-3-chloropyridin-4-yl)oxy-3-fluorophenyl]-5-(4-fluorophenyl)-4-oxo-1H-pyridine-3-carboxamide | ||
| Canonical SMILES | C1=CC(=CC=C1C2=CNC=C(C2=O)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F)F | ||
| Formula | C23H15ClF2N4O3 | M.Wt | 468.84 |
| Solubility | ≥ 23.45mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1329 mL | 10.6646 mL | 21.3292 mL |
| 5 mM | 0.4266 mL | 2.1329 mL | 4.2658 mL |
| 10 mM | 0.2133 mL | 1.0665 mL | 2.1329 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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