1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. Glumetinib

Glumetinib  (Synonyms: Gumarontinib; SCC244)

Cat. No.: HY-116000 Purity: 98.30%
COA Handling Instructions

Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity.

For research use only. We do not sell to patients.

Glumetinib Chemical Structure

Glumetinib Chemical Structure

CAS No. : 1642581-63-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 150 In-stock
Solid
5 mg USD 149 In-stock
10 mg USD 231 In-stock
50 mg USD 589 In-stock
100 mg USD 952 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Glumetinib

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity[1].

IC50 & Target

IC50: 0.42 nM (c-Met kinase)[1]

In Vitro

Glumetinib (SCC244) (0-10 nM; 72 hours) elicits selective and profound effects against c-Met–driven cancer cell proliferation[1].
Glumetinib (0-50 nM; 24 hours) induces G1–S phase cell-cycle arrest in c-Met–addicted human cancer cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: EBC-1, SNU-5, MKN-45, BaF3/TPR-Met cells
Concentration: 0-10 nM
Incubation Time: 72 hours
Result: Specifically and potently inhibited proliferation of c-Met–addicted human cancer cells (IC50 ranging 0.5 to 2.45 nM for EBC-1, SNU-5, MKN-45, BaF3/TPR-Met cells ).

Cell Cycle Analysis[1]

Cell Line: EBC-1 and MKN-45 cells
Concentration: 0-50 nM
Incubation Time: 24 hours
Result: Consistently induced G1–S cell-cycle arrest.
In Vivo

Glumetinib (2.5-10 mg/kg; p.o.; once daily for 2-3 weeks) significantly inhibits c-Met–driven tumor growth in cancer CDX models[1].
Glumetinib shows significant antitumor efficiency in NSCLC and HCC tumor PDX models with MET aberration[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice (4-6 weeks old) (MKN-45 model)[1]
Dosage: 10, 5, 2.5 mg/kg
Administration: P.o.; once daily for 2-3 weeks
Result: Significantly inhibited tumor growth with inhibitory rates of 99.3%, 88.6%, and 63.6% at doses of 10, 5, and 2.5 mg/kg, respectively.
Clinical Trial
Molecular Weight

459.48

Formula

C21H17N9O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(N1N=CC2=NC=C(C3=CN(C)N=C3)C=C21)(C4=CN=C5C=CC(C6=CN(C)N=C6)=CN54)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (90.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1764 mL 10.8819 mL 21.7637 mL 54.4093 mL
5 mM 0.4353 mL 2.1764 mL 4.3527 mL 10.8819 mL
10 mM 0.2176 mL 1.0882 mL 2.1764 mL 5.4409 mL
15 mM 0.1451 mL 0.7255 mL 1.4509 mL 3.6273 mL
20 mM 0.1088 mL 0.5441 mL 1.0882 mL 2.7205 mL
25 mM 0.0871 mL 0.4353 mL 0.8705 mL 2.1764 mL
30 mM 0.0725 mL 0.3627 mL 0.7255 mL 1.8136 mL
40 mM 0.0544 mL 0.2720 mL 0.5441 mL 1.3602 mL
50 mM 0.0435 mL 0.2176 mL 0.4353 mL 1.0882 mL
60 mM 0.0363 mL 0.1814 mL 0.3627 mL 0.9068 mL
80 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6801 mL
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Glumetinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Glumetinib
Cat. No.:
HY-116000
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