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 화학구조

CAS No. : 443798-09-2

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3-Methylthienyl-carbonyl-JNJ-7706621 Related Antibodies

Top Publications Citing Use of Products

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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GSK-3 GSK-3α GSK-3β

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

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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 3
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]
A-375 IC50
0.25 3
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 3
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]
HCT-116 IC50
0.13 3
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 3
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]
HeLa IC50
0.091 3
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 3
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]
MDA-MB-231 IC50
0.55 3
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 3
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]
PC-3 IC50
0.11 3
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 3
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]
SK-OV-3 IC50
0.24 3
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]
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].

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

3-Methylthienyl-carbonyl-JNJ-7706621 Related Antibodies
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].

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.
분자량

378.43

화학식

C14H14N6O3S2
CAS No.
SMILES

O=S(C1=CC=C(NC2=NN(C(C3=C(C)C=CS3)=O)C(N)=N2)C=C1)(N)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
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3-Methylthienyl-carbonyl-JNJ-7706621 Related Classifications

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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
Cat. No.:
HY-141685
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