2. Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK
  3. CDK GSK-3 VEGFR FGFR
  4. 3-Methylthienyl-carbonyl-JNJ-7706621

3-Methylthienyl-carbonyl-JNJ-7706621 

目录号: HY-141685
产品使用指南

摩尔计算器

3-Methylthienyl-carbonyl-JNJ-7706621 是一种有效和选择性的细胞周期蛋白依赖性激酶 (CDK) 抑制剂，对 CDK1/cyclin B 和 CDK2/cyclin A 的 IC50 值分别为 6.4 nM 和 2 nM。3-Methylthienyl-carbonyl-JNJ-7706621 还显示出对 GSK-3 (IC50=0.041 μM) 的有效抑制和对 CDK4，VEGF-R2，and FGF-R2 (IC50=0.11, 0.13, 0.22 μM) 的适度效力。3-Methylthienyl-carbonyl-JNJ-7706621 可用于癌症的研究。

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3-Methylthienyl-carbonyl-JNJ-7706621 Chemical Structure

3-Methylthienyl-carbonyl-JNJ-7706621 Chemical Structure

CAS No. : 443798-09-2

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3-Methylthienyl-carbonyl-JNJ-7706621 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

查看 GSK-3 亚型特异性产品:

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GSK-3 GSK-3α GSK-3β

查看 VEGFR 亚型特异性产品:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 FGFR 亚型特异性产品:

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC50s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer[1].

IC50 & Target[1]

CDK2/cyclinA

2 nM (IC50)

CDK1/cyclinB

6.4 nM (IC50)

GSK3

41 nM (IC50)

CDK4

0.11 μM (IC50)

VEGFR2

0.13 μM (IC50)

FGFR2

0.22 μM (IC50)

体外研究
(In Vitro)

3-Methylthienyl-carbonyl-JNJ-7706621 shows potent potency against GSK-3 (IC50=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC50=0.11, 0.13, 0.22 μM, respectively)[1].
3-Methylthienyl-carbonyl-JNJ-7706621 inhibits cell proliferation, with IC50s of 0.28 μM, 0.25 μM, 0.45 μM, 0.75 μM, 0.59 μM and 0.12 μM for HeLa, HCT-116, A375, SK-OV-3, MDA-MB-231 and PC-3 cells, respectively[1].

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

3-Methylthienyl-carbonyl-JNJ-7706621 相关抗体:
体内研究
(In Vivo)

3-Methylthienyl-carbonyl-JNJ-7706621 (75-125 mg/kg; i.p. once daily for 32 days) inhibits the A375 human melanoma tumor growth and prolongs the survival in nude mice[1].
3-Methylthienyl-carbonyl-JNJ-7706621 exhibits oral bioavailability (nude mouse 2%, rat 8%, dog 63.3%), terminal elimination half-lives (nude mouse 1.70, rat 2.20 and, dog 2.36 h) and Cmax (nude mouse 0.21, rat 2.5, dog 4.58 μM) following oral administration (nude mouse 30, rat 30 , dog 10 mg/kg)[1].
3-Methylthienyl-carbonyl-JNJ-7706621 exhibits terminal elimination half-lives (nude mouse 0.51, rat 0.64 and, dog 3.89 h), Cmax (nude mouse 6.4, rat 23.2, dog 2.19 μM) and AUC (nude mouse 3.2, rat 11.4, dog 2.45 μM•h) following intravenous administration (nude mouse 3, rat 3 and, dog 1 mg/kg)[1].

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

Animal Model: Male athymic mice were implanted with A375 human melanoma cells[1]
Dosage: 75, 100, 125 mg/kg
Administration: I.p. once daily for 32 days
Result: Reduced the tumor growth.
Survival was increased by about 3 weeks compared with vector alone.
分子量

378.43

Formula

C14H14N6O3S2
CAS 号
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

3-Methylthienyl-carbonyl-JNJ-7706621 相关分类

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  • 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:

3-Methylthienyl-carbonyl-JNJ-7706621443798-09-2CDKGSK-3VEGFRFGFRCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Vascular endothelial growth factor receptorFibroblast growth factor receptorcyclin-dependentkinaseCDK1/cyclin?BCDK2/cyclin?ACDK4VEGF-R2FGF-R2cancerInhibitorinhibitorinhibit

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