Glumetinib
Based on 2 publication(s) in Google Scholar
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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- 純度: 99.94%
- CAS 番号: 1642581-63-2
- 分子式: C21H17N9O2S
- 分子量:459.48
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Glumetinib
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生物活性
IC50: 0.42 nM (c-Met kinase)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| EBC-1 | IC50 |
5 nM
Compound: 6
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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
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[PMID: 37262349] |
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.
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Cell Line:EBC-1, SNU-5, MKN-45, BaF3/TPR-Met cells
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Concentration:0-10 nM
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Incubation Time:72 hours
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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 ).
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Cell Line:EBC-1 and MKN-45 cells
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Concentration:0-50 nM
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Incubation Time:24 hours
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Result:Consistently induced G1–S cell-cycle arrest.
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.
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Animal Model:Female nude mice (4-6 weeks old) (MKN-45 model)[1]
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Dosage:10, 5, 2.5 mg/kg
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Administration:P.o.; once daily for 2-3 weeks
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1642581-63-2
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性状 Solid
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分子量 459.48
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分子式 C21H17N9O2S
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Color White to off-white
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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
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別名
Gumarontinib; SCC244
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Dev Cell
A feedback loop between lamellipodial extension and HGF-ERK signaling specifies leader cells during collective cell migration. [Abstract]2022 Oct 10;57(19):2290-2304.e7. PMID: 36174555 -
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
Glumetinib 関連分類
HY-116000 関連分類
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