| Size | Price | Stock | Qty |
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| 1mg |
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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)
BMS-2 (MET Kinase-IN-4) inhibits Met kinase with an IC50 of 1.9 nM. It also targets Flt-3 (IC50 = 4 nM) and 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].
BMS-2 exhibits potent Met kinase inhibition (IC50 = 1.9 nM). At 3 μM, it demonstrates high stability in both human and mouse liver microsomes, indicating favorable metabolic stability. Additionally, it suppresses Flt-3 and VEGFR-2 with IC50 values of 4 nM and 27 nM, respectively. |
| 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.
In mice, BMS-2 shows broad extravascular distribution and a favorable half-life. In GTL-16 human scaffold xenograft models, it exhibits significant dose-dependent antitumor activity when administered orally at doses of 6.25, 12.5, 25, and 50 mg/kg once daily. |
| Enzyme Assay |
Met kinase inhibition was quantified using enzymatic assays. Recombinant Met kinase was incubated with BMS-2 and ATP, followed by detection of phosphorylated substrates. IC50 values were calculated from dose-response curves.
Similar assays were applied for Flt-3 and VEGFR-2 to determine inhibition kinetics and selectivity profiles. |
| Cell Assay |
Antiproliferative activity was evaluated in cancer cell lines dependent on Met signaling. Cells were treated with BMS-2 for 72 hours, and viability was measured using ATP-based luminescence assays.
Mechanistic studies included Western blotting to assess phosphorylation levels of Met and downstream effectors (e.g., ERK, AKT) post-treatment. |
| 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. Pharmacokinetics: Mice received single doses of BMS-2 (5 or 10 mg/kg) intravenously (IV) or orally (PO). Blood samples were collected at intervals for plasma concentration analysis. Efficacy: Nude mice bearing GTL-16 xenografts were orally administered BMS-2 (6.25–50 mg/kg) once daily. Tumor volume and body weight were monitored for 21 days. The compound was formulated in 10% DMSO + 90% corn oil for oral delivery. |
| ADME/Pharmacokinetics |
BMS-2 shows good oral bioavailability and broad extravascular distribution in mice. Half-life (t1/2) and clearance were characterized but not numerically specified.
High stability in liver microsomes suggests low metabolic clearance. |
| Toxicity/Toxicokinetics |
No acute toxicity was observed in mice after a single oral dose of 500 mg/kg. In repeat-dose studies (90 days), histopathological examination of major organs (liver, kidney) showed no abnormalities.
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| References | |
| Additional Infomation |
BMS-2 is an orally bioavailable Met kinase inhibitor developed for cancer research. Its molecular formula is C25H16F2N4O3 (MW: 458.42 g/mol). Solubility in DMSO is ~100 mg/mL (218.14 mM). For in vivo studies, it is solubilized in 10% DMSO + 90% corn oil.
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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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| PubChem CID |
21081761
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
701.5ºC at 760 mmHg
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| Melting Point |
212-214ºC
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| Flash Point |
378.1ºC
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| Index of Refraction |
1.721
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| LogP |
4.82
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
34
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| Complexity |
829
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C(=O)N(C2C=CC(F)=CC=2)C=CC=1)NC1C=C(F)C(OC2C3=C(NC=C3)N=CC=2)=CC=1
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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; 1-(4-fluorophenyl)-N-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-2-oxo-1,2-dihydropyridine-3-carboxamide; N-(3-fluoro-4-{1H-pyrrolo[2,3-b]pyridin-4-yloxy}phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide; 1-(4-fluorophenyl)-N-(3-fluoro-4-(1H-pyrrolo(2,3-b)pyridin-4-yloxy)phenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide; N-(3-fluoro-4-(1H-pyrrolo(2,3-b)pyridin-4-yloxy)phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide; 888719-03-7; N-(4-((1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)-3-fluorophenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide; 1-(4-fluorophenyl)-N-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-2-oxopyridine-3-carboxamide; 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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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