| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
Met (IC50 = 1.9 nM); Flt-3 (IC50 = 4 nM); VEGFR-2 (IC50 = 27 nM)
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| ln Vitro |
MET Kinase-IN-4 (Compound 2) exhibits strong Met inhibitory action, with an IC50 of 1.9 nM [1]. Flt-3 and VEGFR-2 regulation are inhibited by MET Kinase-IN-4, with IC50 values of 4 and 27, respectively. Human and mouse liver microsomes show high stability when MET Kinase-IN-4 (3 μM) is added [1].
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| ln Vivo |
In mice, MET kinase-IN-4 (compound 2) exhibits favorable pharmacokinetic properties [1]. The GTL-16 human scaffold xenograft model showed notable in vivo tumor anti-activity for MET kinase-IN-4.
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| Animal Protocol |
Animal/Disease Models: Mouse [1]
Doses: 5, 10 mg/kg Route of Administration: IV, PO Experimental Results: Exhibits broad extravascular distribution and good half-life. Animal/Disease Models: Nude mice [1] Doses: 6.25, 12.5, 25 and 50 mg/kg Route of Administration: Orally, one time/day Experimental Results: Displayed dose-dependent anti-tumor activity. |
| References |
[1]. Kyoung Soon Kim, et al. Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem. 2008 Sep 11;51(17):5330-41.
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| Molecular Formula |
C25H16F2N4O3
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|---|---|
| Molecular Weight |
458.42
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| Exact Mass |
458.119
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| Elemental Analysis |
C, 65.50; H, 3.52; F, 8.29; N, 12.22; O, 10.47
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| CAS # |
888719-03-7
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| Related CAS # |
888719-03-7
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| Appearance |
Solid powder
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| SMILES |
C1=CN(C(=O)C(=C1)C(=O)NC2=CC(=C(C=C2)OC3=C4C=CNC4=NC=C3)F)C5=CC=C(C=C5)F
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| InChi Key |
OBSFXHDOLBYWRJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H16F2N4O3/c26-15-3-6-17(7-4-15)31-13-1-2-19(25(31)33)24(32)30-16-5-8-22(20(27)14-16)34-21-10-12-29-23-18(21)9-11-28-23/h1-14H,(H,28,29)(H,30,32)
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| Chemical Name |
1-(4-fluorophenyl)-N-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-2-oxopyridine-3-carboxamide
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| Synonyms |
BMS-2; BMS 2; BMS2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~218.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1814 mL | 10.9070 mL | 21.8141 mL | |
| 5 mM | 0.4363 mL | 2.1814 mL | 4.3628 mL | |
| 10 mM | 0.2181 mL | 1.0907 mL | 2.1814 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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