JNJ7706621
JNJ-7706621
CAS: 443797-96-4
Molecular Formula: C15H12F2N6O3S
JNJ7706621 - Names and Identifiers
JNJ7706621 - Physico-chemical Properties
| Molecular Formula | C15H12F2N6O3S |
| Molar Mass | 394.36 |
| Density | 1.71 |
| Melting Point | 149-155℃ |
| Boling Point | 676.6±65.0 °C(Predicted) |
| Solubility | Soluble in DMSO at 15mg/ml |
| Appearance | White solid |
| pKa | 9.80±0.12(Predicted) |
| Storage Condition | +2C to +8C |
| Sensitive | Light Sensitive |
| In vitro study | JNJ-7706621 was highly effective at CDK1 and 2 with an IC50 of 3-9 nM. JNJ-7706621 also inhibited CDK3, 4, and 6 with an IC50 of 58-253 nM. JNJ-7706621 inhibition of Aurora-A and B,IC50 were 11 and 15 nM, respectively. JNJ-7706621 also inhibited VEGF-R2,FGF-R2, and GSK3β with an IC50 of -254 nM. JNJ-7706621 inhibits a panel of human cancer cells, including HeLa,HCT-116,SK-OV-3,PC3,DU145,A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with an IC50 of 112-514 nM. JNJ-7706621 inhibition of the growth of normal cell lines, including MRC-5, HASMC, HUVEC, and HMVEC was several times less effective with an IC50 of 3.67-5.42 μm. 0.5-3 μm JNJ-7706621 acts on HeLa or U937 cells to arrest the cells in the G2-M phase, induce nuclear replication, activate apoptosis, and reduce colony formation. JNJ-7706621 is highly effective at CDK1 and 2 with an IC50 of 3-9 nM. JNJ-7706621 also inhibited CDK3, 4, and 6 with an IC50 of 58-253 nM. JNJ-7706621 inhibition of Aurora-A and B,IC50 were 11 and 15 nM, respectively. JNJ-7706621 also inhibited VEGF-R2,FGF-R2, and GSK3β with an IC50 of -254 nM. JNJ-7706621 inhibits a panel of human cancer cells, including HeLa,HCT-116,SK-OV-3,PC3,DU145,A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with an IC50 of 112-514 nM. JNJ-7706621 inhibition of the growth of normal cell lines, including MRC-5, HASMC, HUVEC, and HMVEC was several times less effective with an IC50 of 3.67-5.42 μm. 0.5-3 μm JNJ-7706621 acts on HeLa or U937 cells to arrest the cells in the G2-M phase, induce nuclear replication, activate apoptosis, and reduce colony formation. |
| In vivo study | 100 or 125 mg/kg JNJ-7706621 treatment of mice bearing A375 malignant melanoma human tumor xenograft model resulted in tumor regression. 100 or 125 mg/kg JNJ-7706621 treatment of mice bearing A375 malignant melanoma human tumor xenograft model resulted in tumor regression. |
JNJ7706621 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.536 ml | 12.679 ml | 25.358 ml |
| 5 mM | 0.507 ml | 2.536 ml | 5.072 ml |
| 10 mM | 0.254 ml | 1.268 ml | 2.536 ml |
| 5 mM | 0.051 ml | 0.254 ml | 0.507 ml |
Last Update：2024-01-02 23:10:35
JNJ7706621 - Reference Information
| biological activity | JNJ-7706621 is a pan-CDK inhibitor with the strongest inhibitory effect on CDK1/2, the IC50 is 9 nM/4 nM and is more than 6-fold more selective for CDK1/2 than for CDK3/4/6. Aurora A/B was also effectively inhibited, with no inhibitory activity on Plk1 and wee1. JNJ-7706621 is a pan-CDK inhibitor with the strongest inhibitory effect on CDK1/2, with an IC50 of 9 nM/4 nM in a cell-free assay, acting on CDK1/2 is more than 6-fold more selective than acting on CDK3/4/6. Aurora A/B was also effectively inhibited, with no inhibitory activity on Plk1 and wee1. |
| in vitro study | JNJ-7706621 is highly effective at CDK1 and 2 with an IC50 of 3-9 nM. JNJ-7706621 also inhibited CDK3, 4, and 6 with an IC50 of 58-253 nM. JNJ-7706621 inhibition of Aurora-A and B,IC50 were 11 and 15 nM, respectively. JNJ-7706621 also inhibited VEGF-R2,FGF-R2, and GSK3β with an IC50 of -254 nM. JNJ-7706621 inhibits a panel of human cancer cells, including HeLa,HCT-116,SK-OV-3,PC3,DU145,A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with an IC50 of 112-514 nM. JNJ-7706621 inhibition of the growth of normal cell lines, including MRC-5, HASMC, HUVEC, and HMVEC was several times less effective with an IC50 of 3.67-5.42 μm. 0.5-3 μm JNJ-7706621 acts on HeLa or U937 cells to arrest the cells in the G2-M phase, induce nuclear replication, activate apoptosis, and reduce colony formation. JNJ-7706621 is highly effective at CDK1 and 2 with an IC50 of 3-9 nM. JNJ-7706621 also inhibited CDK3, 4, and 6 with an IC50 of 58-253 nM. JNJ-7706621 inhibition of Aurora-A and B,IC50 were 11 and 15 nM, respectively. JNJ-7706621 also inhibited VEGF-R2,FGF-R2, and GSK3β with an IC50 of -254 nM. JNJ-7706621 inhibits a panel of human cancer cells, including HeLa,HCT-116,SK-OV-3,PC3,DU145,A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with an IC50 of 112-514 nM. JNJ-7706621 inhibition of the growth of normal cell lines, including MRC-5, HASMC, HUVEC, and HMVEC was several times less effective with an IC50 of 3.67-5.42 μm. 0.5-3 μm JNJ-7706621 acts on HeLa or U937 cells to arrest the cells in the G2-M phase, induce nuclear replication, activate apoptosis, and reduce colony formation. |
| in vivo study | mice bearing A375 malignant melanoma human tumor xenograft model treated with 100 or 125 mg/kg JNJ-7706621, resulting in tumor regression. 100 or 125 mg/kg JNJ-7706621 treatment of mice bearing A375 malignant melanoma human tumor xenograft model resulted in tumor regression. |
| signature | JNJ-7706621 is a novel potent inhibitor of a broad spectrum of CDKs and Aurora kinases. |
| Target | TargetValue CDK2/CyclinE (Cell-free assay) 3 nM CDK2/cyclin A (Cell-free assay) 4 nM CDK1/CyclinB (Cell-free assay) 9 nM Aurora A (Cell-free assay) 11 nM Aurora B (Cell-free assay) 15 nM |
| Target | Value |
| CDK2/CyclinE (Cell-free assay) | 3 nM |
| CDK2/CyclinA (Cell-free assay) | 4 nM |
| CDK1/CyclinB (Cell-free assay) | 9 nM |
| Aurora A (Cell-free assay) | 11 nM |
| Aurora B (Cell-free assay) | 15 nM |
Last Update：2024-04-09 20:52:54
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Spot supply
Product Name: JNJ-7706621 Visit Supplier Webpage Request for quotationCAS: 443797-96-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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