2. Protein Tyrosine Kinase/RTK Apoptosis
  3. c-Met/HGFR Apoptosis
  4. c-Met-IN-22

c-Met-IN-22（compound 51am） 是一种口服有效的 c-Met 抑制剂，IC50 值是 2.54 nM。c-Met-IN-22 具有抗增殖活性和抗肿瘤活性。c-Met-IN-22 可以诱导细胞凋亡（apoptosis）。

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c-Met-IN-22 Chemical Structure

c-Met-IN-22 Chemical Structure

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Customer Review

c-Met-IN-22 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

c-Met-IN-22 (compound 51am) is an orally active inhibitor against c-Met with an IC50 value of 2.54 nM. c-Met-IN-22 has antiproliferative and antitumor activities. c-Met-IN-22 induces cell apoptosis[1].

IC50 & Target[1]

c-Metwild type

2.54 nM (IC50)

c-MetH1094R

93.6 nM (IC50)

c-MetD1228H

29.4 nM (IC50)

c-MetY1230H

45.8 nM (IC50)

c-MetY1235D

54.2 nM (IC50)

c-MetM1250T

26.5 nM (IC50)

c-Metkit

4.94 nM (IC50)

c-MetRon

3.83 nM (IC50)

c-MetPDGFRα

425 nM (IC50)

c-MetPDGFRβ

513 nM (IC50)

c-MetVEGFR-2

527 nM (IC50)

c-MetFit-3

6.12 nM (IC50)

c-MetFit-4

276 nM (IC50)

体外研究
(In Vitro)

c-Met-IN-22 在细胞 MNK-45，A-549，HT-29，MDA-MB-231，HUVEC 和 FHC 中具有抗增殖活性，IC50 值分别为0.092，0.83，0.68，3.94，2.54 和 8.63 μM[1]。
c-Met-IN-22 对突变体 H1094R，D1228H，Y1230H，Y1235D 和 M1250T 仍具有抑制作用，IC50 值分别为 93.6，29.4，45.8，54.2 和 26.5 nM[1]。
c-Met-IN-22（0，2.5， 5.0 和 10.0 μM； 24 h）具有剂量依赖性的抑制 MKN-45 中 c-Met 的磷酸化[1]。
c-Met-IN-22（0.4，0.8 和 1.2  μM；24 h）诱导 MNK-45 细胞周期在 G2 阶段的阻滞和细胞凋亡，且具有剂量依赖性[1]。

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

c-Met-IN-22 相关抗体:

Apoptosis Analysis[1]

Cell Line: MNK- 45 cells
Concentration: 0.4, 0.8, 1.2 μM
Incubation Time: 24 h
Result: Induced cell apoptosis in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: MNK- 45 cells
Concentration: 0.4, 0.8, 1.2 μM
Incubation Time: 24 h
Result: Induced cell cycle arrest at G2 phase in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MNK- 45 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Inhibited c-Met phosphorylation in a dose-dependent manner.
体内研究
(In Vivo)

c-Met-IN-22（10mg/kg；口服；单剂量）在 BALB/c 小鼠中表现出良好的口服生物利用度（F=69%），清除半衰期是 5.6 小时，清除率是 0.87L/h•kg [1]。
c-Met-IN-22（1.5mg/kg，静脉注射）在 BALB/c 小鼠中的清除半衰期是 3.2 小时[1]。

c-Met-IN-22 在 BALB/c 小鼠体内的药代动力学分析[1]

Route Dose (mg/kg) AUC0→∞ (μg·h/mL) T1/2 (h) Tmax (h) Cmax (ng/mL) Cl (L/h·kg) F (%)
i.v. 1.5mg/kg 2.5 3.2 / 552 0.6 /
p.o. 10mg/kg 11.5 5.6 4.1 1756 / 69

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

Animal Model: Pharmacokinetic Analysis in BALB/c mice
Dosage: p.o.10 mg/kg; i.v. 1.5 mg/kg
Administration: Intravenous (i.v.) injection, Oral administration (p.o.)
Result: Characterised good maximum concentration, plasma exposure and elimination half-time in pharmacokinetics.
分子量

512.74

Formula

C21H10Cl3F2N3O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

c-Met-IN-22 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

c-Met-IN-22c-Met/HGFRApoptosisc-MetBALB/c mice MNK-45A-549HT-29MDA-MB-231HUVECFHCInhibitorinhibitorinhibit

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