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.
For research use only. We do not sell to patients.
- CAS No.: 443798-09-2
- Formula: C14H14N6O3S2
- Molecular Weight:378.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
0.25 μM
Compound: 3f
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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
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[PMID: 15974571] |
| HCT-116 | IC50 |
0.13 μM
Compound: 3f
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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
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[PMID: 15974571] |
| HeLa | IC50 |
0.091 μM
Compound: 3f
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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
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[PMID: 15974571] |
| MDA-MB-231 | IC50 |
0.55 μM
Compound: 3f
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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
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[PMID: 15974571] |
| PC-3 | IC50 |
0.11 μM
Compound: 3f
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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
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[PMID: 15974571] |
| SK-OV-3 | IC50 |
0.24 μM
Compound: 3f
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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
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[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.
In Vivo
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.
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Animal Model:Male athymic mice were implanted with A375 human melanoma cells[1]
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Dosage:75, 100, 125 mg/kg
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Administration:I.p. once daily for 32 days
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Result:Reduced the tumor growth.
Survival was increased by about 3 weeks compared with vector alone.
Chemical Information
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CAS No. 443798-09-2
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Molecular Weight 378.43
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Formula C14H14N6O3S2
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SMILES
O=S(C1=CC=C(NC2=NN(C(C3=C(C)C=CS3)=O)C(N)=N2)C=C1)(N)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
3-Methylthienyl-carbonyl-JNJ-7706621 Related Classifications
HY-141685 Related Classifications
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