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 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.

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3-Methylthienyl-carbonyl-JNJ-7706621

3-Methylthienyl-carbonyl-JNJ-7706621 構造式

CAS 番号 : 443798-09-2

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3-Methylthienyl-carbonyl-JNJ-7706621 関連抗体

Top Publications Citing Use of Products

CDK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

GSK-3 アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
GSK-3 GSK-3α GSK-3β

VEGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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製品説明

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)

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
0.25 μM
Compound: 3f
In vitro inhibitory concentration against cell proliferation in human A375 (malignant melanoma),tumor cells
In vitro inhibitory concentration against cell proliferation in human A375 (malignant melanoma),tumor cells
[PMID: 15974571]
HCT-116 IC50
0.13 μM
Compound: 3f
In vitro inhibitory concentration against cell proliferation in human HCT116 (colon carcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in human HCT116 (colon carcinoma) tumor cells
[PMID: 15974571]
HeLa IC50
0.091 μM
Compound: 3f
In vitro inhibitory concentration against cell proliferation in human HeLa (cervical adenocarcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in human HeLa (cervical adenocarcinoma) tumor cells
[PMID: 15974571]
MDA-MB-231 IC50
0.55 μM
Compound: 3f
In vitro inhibitory concentration against cell proliferation in various human MDA-MB-231 (breast carcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in various human MDA-MB-231 (breast carcinoma) tumor cells
[PMID: 15974571]
PC-3 IC50
0.11 μM
Compound: 3f
In vitro inhibitory concentration against cell proliferation in human PC-3 (prostate adenocarcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in human PC-3 (prostate adenocarcinoma) tumor cells
[PMID: 15974571]
SK-OV-3 IC50
0.24 μM
Compound: 3f
In vitro inhibitory concentration against cell proliferation in human SK-OV-3 (ovarian adenocarcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in human SK-OV-3 (ovarian adenocarcinoma) tumor cells
[PMID: 15974571]
体外実験

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].

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

3-Methylthienyl-carbonyl-JNJ-7706621 関連抗体
体内実験

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].

MedChemExpress (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

分子式

C14H14N6O3S2
CAS 番号
SMILES

O=S(C1=CC=C(NC2=NN(C(C3=C(C)C=CS3)=O)C(N)=N2)C=C1)(N)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
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3-Methylthienyl-carbonyl-JNJ-7706621 Related Classifications

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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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3-Methylthienyl-carbonyl-JNJ-7706621
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