Capmatinib HCl hydrate (INCB-28060; INC280)

Alias: Capmatinib hydrochloride; INC 280; INCB028060; INCB-028060; INCB 028060; INCB28060; INCB-28060; INCB 28060; Capmatinib; NVP-INC 280AAA; INC280; INC-280
Cat No.:V2201 Purity: ≥98%
CapmatinibHCl hydrate (INCB28060; INC-280) is a n FDA-approved, orally bioavailable, ATP-competitive inhibitor of c-MET (IC50 = 0.13 nM in a cell-free assay) with anticancer activity.
Capmatinib HCl hydrate (INCB-28060; INC280) Chemical Structure CAS No.: 1865733-40-9
Product category: c-MET
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of Capmatinib HCl hydrate (INCB-28060; INC280):

  • Capmatinib (INCB28060; INC-280)
  • Capmatinib 2HCl
  • Capmatinib HCl
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Capmatinib HCl hydrate (INCB28060; INC-280) is a n FDA-approved, orally bioavailable, ATP-competitive inhibitor of c-MET (IC50 = 0.13 nM in a cell-free assay) with anticancer activity. It is not active against EGFR, HER-3, or RONβ. By binding to c-Met specifically, the c-Met inhibitor INC280 prevents c-Met phosphorylation and obstructs c-Met signal transduction pathways. When tumor cells overexpress c-Met protein or express constitutively activated c-Met protein, this may result in cell death.

Biological Activity I Assay Protocols (From Reference)
Targets
c-MET (IC50 = 0.13 nM)
ln Vitro

INCB28060 has more than 10,000-fold selectivity over a broad panel of human kinases, picomolar enzymatic potency, and high specificity for c-MET. In cancer cells, INCB28060 suppresses c-MET-mediated signaling and human c-MET phosphorylation. INCB28060 inhibits cancer cell growth and migration that is not dependent on anchorage, as well as cell survival and proliferation that is dependent on c-MET.[1]

ln Vivo
INCB28060 demonstrates potent antitumor activity in tumor models in mice dependent on c-MET; oral administration of 0.03 mg/kg INCB28060 results in a 50% reduction in c-MET phosphorylation. In mice exhibiting tumors, there is observed a dose-dependent inhibition of tumor growth.[1]
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
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.
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.
References

[1]. Clin Cancer Res . 2011 Nov 15;17(22):7127-38.

[2]. BMC Res Notes . 2019 Mar 11;12(1):125.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H21CL2FN6O2
Molecular Weight
503.3594
Exact Mass
502.1087075
Elemental Analysis
C, 54.88; H, 4.21; Cl, 14.09; F, 3.77; N, 16.70; O, 6.36
CAS #
1865733-40-9
Appearance
Solid powder
SMILES
CNC(=O)C1=C(C=C(C=C1)C2=NN3C(=CN=C3N=C2)CC4=CC5=C(C=C4)N=CC=C5)F.O.Cl.Cl
InChi Key
COWBUPJEEDYWKD-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H17FN6O.2ClH.H2O/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);2*1H;1H2
Chemical Name
2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide;hydrate;dihydrochloride
Synonyms
Capmatinib hydrochloride; INC 280; INCB028060; INCB-028060; INCB 028060; INCB28060; INCB-28060; INCB 28060; Capmatinib; NVP-INC 280AAA; INC280; INC-280
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~20.83 mg/mL (~41.38 mM)
H2O : ~3.33 mg/mL (~6.62 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9866 mL 9.9332 mL 19.8665 mL
5 mM 0.3973 mL 1.9866 mL 3.9733 mL
10 mM 0.1987 mL 0.9933 mL 1.9866 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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • Capmatinib (INCB28060)

    INCB28060 inhibits c-MET–dependent cell proliferation and survival. Clin Cancer Res. 2011 Nov 15;17(22):7127-38.

  • Capmatinib (INCB28060)

    HGF induces production of TGF-α, AR, and HRG-β1 in cancer cells and INCB28060 effectively blocks the induction.

  • Capmatinib (INCB28060)

    Cross-talk between c-MET and EGFR or HER-3 in cancer cells.

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