| 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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| 500mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
Wnt/β-catenin; c-Met (IC50 = 0.13 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The assay buffer has the following contents: pH 7.8, 50 mM Tris-HCl, 10 mM MgCl2, 100 mM NaCl, 0.1 mg/ml BSA, and 5 mM DTT. Spotted on 384-well plates for HTS are 0.8 μL of 5 mM INCB28060 dissolved in DMSO. According to DMSO titration, a solvent concentration of 4% is the highest that can be tolerated. The INCB28060 plate is prepared by serial dilutions at three and eleven points in order to measure IC50s. The assay plate is transferred with 0.8 μL of INCB28060 in DMSO from the INCB28060 plate. DMSO has a final concentration of 2%. In assay buffer, solutions of 0.5 nM phosphorylated c-Met or 8 nM unphosphorylated c-Met are made. In an assay buffer containing 400 μM ATP (unphosphorylated c-Met) or 160 uM ATP (phosphorylated c-Met), a 1 mM stock solution of the peptide substrate Biotin-EQEDEPEGDYFEWLE-amide dissolved in DMSO is diluted to 1 μM. To start the reaction, add 20 μL of substrate solution per well after adding a 20 μL volume of enzyme solution (or assay buffer for the enzyme blank) to the corresponding wells in each plate. For ninety minutes, the plate is incubated at 25 °C with protection from light. To terminate the reaction, introduce 20 μL of a mixture comprising 45 mM EDTA, 50 mM Tris-HCl, 50 mM NaCl, 0.4 mg/ml BSA, 200 nM SA-APC, and 3 nM EUPy20. After incubating the plate at room temperature for 15-30 minutes, the Perkin Elmer Fusion α-FP instrument measures the homogenous time resolved fluorescence (HTRF). The following HTRF program settings are in use: 330/30 primary excitation filter 200 uSec for the primary window, 50 uSec for the primary delay, and 15 flashes total. Time to read well: 2000
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| Cell Assay |
In RPMI-1640 medium with 10% FBS, H441 cells are seeded and grown to full confluence. Using a P200 pipette tip, cells are scraped to create gaps. Next, in the presence of varied INCB28060 concentrations, cells are stimulated with 50 ng/mL recombinant human HGF to induce migration across the gap. Following an overnight incubation period, a semiqualitative evaluation of the inhibition of cell migration is carried out and representative photos are taken.
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| Animal Protocol |
Eight-week-old female Balb/c nu/nu mice (Charles River) are inoculated subcutaneously with 4 × 106 tumor cells (S114 model) or with 5 × 106 tumor cells (U-87MG glioblastoma model).
3, 10, 30 mg/kg INCB28060 is orally dosed, twice each day. |
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| References |
| Molecular Formula |
C23H17FN6O
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| Molecular Weight |
412.42
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| Exact Mass |
412.14
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| Elemental Analysis |
C, 66.98; H, 4.15; F, 4.61; N, 20.38; O, 3.88
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| CAS # |
1029712-80-8
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| Related CAS # |
Capmatinib dihydrochloride hydrate;1865733-40-9;Capmatinib dihydrochloride;1197376-85-4;Capmatinib hydrochloride;1029714-89-3
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| Appearance |
Yellow solid powder
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| SMILES |
CNC(=O)C1=C(C=C(C=C1)C2=NN3C(=CN=C3N=C2)CC4=CC5=C(C=C4)N=CC=C5)F
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| InChi Key |
LIOLIMKSCNQPLV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H17FN6O/c1-25-22(31)18-6-5-16(11-19(18)24)21-13-28-23-27-12-17(30(23)29-21)10-14-4-7-20-15(9-14)3-2-8-26-20/h2-9,11-13H,10H2,1H3,(H,25,31)
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| Chemical Name |
2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
5%DMSO+40%PEG300+5%Tween80+50%ddH2O: 6mg/ml (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4247 mL | 12.1236 mL | 24.2471 mL | |
| 5 mM | 0.4849 mL | 2.4247 mL | 4.8494 mL | |
| 10 mM | 0.2425 mL | 1.2124 mL | 2.4247 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04427072 | Active Recruiting |
Drug: Capmatinib Drug: Docetaxel |
Carcinoma, Non-Small-Cell Lung | Novartis Pharmaceuticals | September 25, 2020 | Phase 3 |
| NCT04926831 | Active Recruiting |
Drug: capmatinib | Non-small Cell Lung Cancer | Novartis Pharmaceuticals | August 10, 2022 | Phase 2 |
| NCT02414139 | Active Recruiting |
Drug: INC280 (capmatinib) |
Carcinoma, Non-Small-Cell Lung | Novartis Pharmaceuticals | June 11, 2015 | Phase 2 |
| NCT03333343 | Active Recruiting |
Drug: INC280 Drug: gefitinib |
EGFR-mutant Non-small Cell Lung Cancer |
Novartis Pharmaceuticals | January 29, 2018 | Phase 1 |
| NCT05703516 | Recruiting | Other: Capmatinib | Non-Small-Cell Lung Carcinoma | Novartis Pharmaceuticals | June 12, 2023 |
INCB28060 inhibits c-MET–dependent cell proliferation and survival. Clin Cancer Res. 2011 Nov 15;17(22):7127-38. |
HGF induces production of TGF-α, AR, and HRG-β1 in cancer cells and INCB28060 effectively blocks the induction. |
Cross-talk between c-MET and EGFR or HER-3 in cancer cells. |
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