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5mg |
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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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Purity: ≥98%
Glumetinib (SCC244; SCC-244; Gumarontinib) is a novel, potent and highly selective c-Met kinase inhibitor (IC50 = 0.42 nM.) with antitumor activity. Remarkably selective compared to 312 other tested protein kinases, glumetinib demonstrated subnanomolar potency against c-Met kinase activity. This makes it one of the most selective c-Met inhibitors currently available. Additionally, the c-Met-dependent neoplastic phenotype of tumor and endothelial cells is suppressed by this inhibitor, which profoundly and specifically inhibits c-Met signal transduction.
Targets |
c-Met kinase (IC50 = 0.42 nM)
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ln Vitro |
SCC244 significantly inhibits the phosphorylation of c-Met, AKT, and ERK in EBC-1, MKN-45 cells with an amplified MET gene, and HGF-stimulated U87MG cells. SCC244 inhibits the proliferation of cancer cells driven by c-Met in a targeted and effective manner. It suppresses angiogenesis and metastasis, two c-Met-dependent neoplastic phenotypes[1].
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ln Vivo |
SCC244 administration shows strong antitumor activity at well-tolerated doses in xenografts of human tumor cell lines, non-small cell lung cancer, and hepatocellular carcinoma patient-derived tumor tissue driven by MET aberration. SCC244 also inhibits c-Met downstream signaling through a mechanism of combined antiproliferation and antiangiogenic effects, which contributes to its in vivo antitumor activity[1].
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Cell Assay |
Prior to a 2-hour treatment with SCC244 and a 15-minute HGF stimulation period, U87MG cells are serum-deprived for a full day. Once the cells are lysed, a Western blot analysis is performed.
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Animal Protocol |
Female nude mice with xenograft tumors
10 mg/kg oral |
References |
Molecular Formula |
C21H17N9O2S
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Molecular Weight |
459.4838
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Exact Mass |
459.12
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Elemental Analysis |
C, 54.89; H, 3.73; N, 27.44; O, 6.96; S, 6.98
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CAS # |
1642581-63-2
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Related CAS # |
1642581-63-2
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Appearance |
Solid powder
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SMILES |
CN1C=C(C=N1)C2=CN3C(=NC=C3S(=O)(=O)N4C5=C(C=N4)N=CC(=C5)C6=CN(N=C6)C)C=C2
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InChi Key |
RYBLECYFLJXEJX-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H17N9O2S/c1-27-11-16(7-24-27)14-3-4-20-23-10-21(29(20)13-14)33(31,32)30-19-5-15(6-22-18(19)9-26-30)17-8-25-28(2)12-17/h3-13H,1-2H3
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Chemical Name |
6-(1-methylpyrazol-4-yl)-1-[6-(1-methylpyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]sulfonylpyrazolo[4,3-b]pyridine
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Synonyms |
SCC-244; SCC244; SCC 244; Gumarontinib.
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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: 11~41.7 mg/mL (23.9~90.7 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1764 mL | 10.8819 mL | 21.7637 mL | |
5 mM | 0.4353 mL | 2.1764 mL | 4.3527 mL | |
10 mM | 0.2176 mL | 1.0882 mL | 2.1764 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 |
NCT04270591 | Recruiting | Drug: Glumetinib | C-Met Exon 14 Mutation | Haihe Biopharma Co., Ltd. | July 15, 2019 | Phase 1 Phase 2 |
NCT05507294 | Completed | Drug: Glumetinib | Healthy Volunteers | Haihe Biopharma Co., Ltd. | March 2, 2021 | Phase 1 |
NCT04797702 | Completed | Combination Product: Glumetinib combined with Toripalimab |
Relapsed or Metastatic Non- small Cell Lung Cancer |
Shanghai Junshi Bioscience Co., Ltd. |
April 15, 2021 | Phase 1 Phase 2 |
SCC244 is a potent and highly selective c-Met inhibitor, with subnanomolar biochemical and nanomolar cellular potency against c-Met. Mol Cancer Ther . 2018 Apr;17(4):751-762. td> |
SCC244 specifically and potently inhibits proliferation of c-Met–addicted human cancer cells. Mol Cancer Ther . 2018 Apr;17(4):751-762. td> |
SCC244 inhibited c-Met–dependent neoplastic phenotypes of metastasis and angiogenesis. Mol Cancer Ther . 2018 Apr;17(4):751-762. td> |
SCC244 significantly inhibited c-Met–driven tumor growth in cancer CDX models. Mol Cancer Ther . 2018 Apr;17(4):751-762. td> |