2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR
  4. MET kinase-IN-2

MET kinase-IN-2 是一种有效的选择性的，具有口服活性的 MET 激酶抑制剂，IC50 值为 7.4 nM。MET kinase-IN-2 具有抗肿瘤活性。

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MET kinase-IN-2 Chemical Structure

MET kinase-IN-2 Chemical Structure

CAS No. : 2101241-90-9

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Customer Review

MET kinase-IN-2 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

MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HT-29 IC50
4.2 μM
Compound: 20j
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 32113049]
MKN-45 IC50
2.9 μM
Compound: 20j
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 32113049]
NCI-H460 IC50
3.6 μM
Compound: 20j
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 32113049]
体外研究
(In Vitro)

MET kinase-IN-2 (compound 20j; 72 hours) inhibits U-87 MG, NIH-H460, HT-29, and MKN-45 cell lines with IC50s ranging 2.9 to 4.5 μM[1].
MET kinase-IN-2 inhibits AXL, Flt4, KDR, Mer, TEK, and TYRO3 with IC50s ranging from 16.5 to 198 nM[1].

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

MET kinase-IN-2 相关抗体:
体内研究
(In Vivo)

MET kinase-IN-2 (3-37.5 mg/kg; p.o.; 7 days per week for 3 weeks) exhibits statistically significant tumor growth inhibition in the U-87 MG 24 xeograft model[1].
MET kinase-IN-2 treatment shows that the Cmax, AUC0-∞, T1/2，CL, and F% values are 1.5 µg/mL, 10.7 µg•h/mL, 4.9 hours, 0.5 L/h/kg, and F=32%, respectively[1].

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

Animal Model: 4-6 weeks old Female nude mice (U-87 MG xenograft model)[1]
Dosage: 3, 6, 12.5, 37.5 mg/kg
Administration: P.o.; 7 days per week for 3 weeks
Result: Induced dose-dependent tumor growth inhibition.
Animal Model: Male SD rats[1]
Dosage: 5 mg/kg
Administration: P.o. (Pharmacokinetic Analysis)
Result: Displayed favorable overall PK profiles, with maximal plasma concentration (Cmax=1.5 µg/mL, 5-fold higher to that of IV), plasma exposure (AUC0-∞=10.7 µg•h/mL, 9.7-fold higher to that of IV), half-life (T1/2=4.9 h, 4.9-fold longer to that of IV), total clearance CL (0.5 L/h/kg; 10-fold lower to that of IV), and oral bioavailability (F=32%, 2.7-fold higher to that of IV) after oral dose of 5 mg/kg (10 mg/kg for IV).
分子量

562.59

Formula

C33H27FN4O4
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

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

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (177.75 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7775 mL 8.8875 mL 17.7749 mL
5 mM 0.3555 mL 1.7775 mL 3.5550 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

MET kinase-IN-2 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7775 mL 8.8875 mL 17.7749 mL 44.4373 mL
5 mM 0.3555 mL 1.7775 mL 3.5550 mL 8.8875 mL
10 mM 0.1777 mL 0.8887 mL 1.7775 mL 4.4437 mL
15 mM 0.1185 mL 0.5925 mL 1.1850 mL 2.9625 mL
20 mM 0.0889 mL 0.4444 mL 0.8887 mL 2.2219 mL
25 mM 0.0711 mL 0.3555 mL 0.7110 mL 1.7775 mL
30 mM 0.0592 mL 0.2962 mL 0.5925 mL 1.4812 mL
40 mM 0.0444 mL 0.2222 mL 0.4444 mL 1.1109 mL
50 mM 0.0355 mL 0.1777 mL 0.3555 mL 0.8887 mL
60 mM 0.0296 mL 0.1481 mL 0.2962 mL 0.7406 mL
80 mM 0.0222 mL 0.1111 mL 0.2222 mL 0.5555 mL
100 mM 0.0178 mL 0.0889 mL 0.1777 mL 0.4444 mL
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:

MET kinase-IN-22101241-90-9c-Met/HGFRselectiveoraltumorantiproliferativeU-87 MGcellsInhibitorinhibitorinhibit

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