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

Glumetinib  (Synonyms: Gumarontinib; SCC244)

Cat. No.: HY-116000 Pureza: 99.94%
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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.

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Glumetinib

Glumetinib Estructura química

No. CAS : 1642581-63-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Based on 2 publication(s) in Google Scholar

Glumetinib Related Antibodies

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Descripciòn

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]
Cellular Effect
Cell Line Type Value Description References
EBC-1 IC50
5 nM
Compound: 6
Antiproliferative activity against human EBC-1 cells assessed as inhibition of cell growth
Antiproliferative activity against human EBC-1 cells assessed as inhibition of cell growth
[PMID: 37262349]
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.

Glumetinib Related Antibodies

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.
Ensayo clínico
Peso molecular

459.48

Fòrmula

C21H17N9O2S
No. CAS
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
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.

  • Calculadora de molaridad

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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Referencias

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.

Keywords:

Glumetinib1642581-63-2Gumarontinib SCC244SCC244SCC 244SCC-244c-Met/HGFRoralbioavailableATP-competitivecancercellproliferationNSCLCHCCtumorInhibitorinhibitorinhibit

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Nombre del producto:
Glumetinib
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