PHA-680632
PHA-680632
CAS: 398493-79-3
Molecular Formula: C28H35N7O2
PHA-680632 - Names and Identifiers
PHA-680632 - Physico-chemical Properties
| Molecular Formula | C28H35N7O2 |
| Molar Mass | 501.62 |
| Density | 1.294 |
| Melting Point | 240-242 °C |
| Boling Point | 709.0±60.0 °C(Predicted) |
| pKa | 12.26±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | PHA-680632 potently inhibits all three Aurora kinases, with IC50 values of 27,135, and 120 nM for Aurora A,B, and C, respectively. PHA-680632 selectively acted on Aurora kinase, The IC50 value was 10 to 200 times higher than that of FGFR1, FLT3,LCK,PLK1,STLK2,VEGFR2, and VEGFR3, the IC50 value is greater than 10 μm when acting on the other 22 kinases. PHA-680632 has antiproliferative effects on a variety of cell lines, including HeLa,HCT116, HT29,LOVO,DU145, and NHDF cells, with an IC50 of 0.06-7.15 μm. The 0.5 μm PHA-680632 acts on tumor cells, causing polyploidy. The mechanism of PHA-680632 activity is consistent with inhibition of Aurora kinase. The combination of PHA-680632 and radiation treatment leads to an enhanced effect on tumor cells, especially on p53-deficient cells. The combination of 100-400 nM PHA680632 and ionizing radiation treatment of p53-deficient HCT116 cells, but not p53 wild-type cells, enhanced radiation-induced annexin V-positive cells, Micronucleus formation, and Brca1 colony formation. |
| In vivo study | PHA-680632 at a dose of 15-60 mg/kg in a mouse model of transplanted tumors carrying HL60,A2780, and HCT116 cells inhibited tumor growth by reducing tumor cell proliferation and promoting apoptosis. PHA-680632 at a dose of 45 mg/kg in transgenic mice carrying mammary tumor virus v-Ha-ras inhibited the growth of mammary tumors driven by activated ras, resulting in the stabilization of all tumors and partial tumor regression. |
PHA-680632 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.993 ml | 9.967 ml | 19.935 ml |
| 5 mM | 0.399 ml | 1.993 ml | 3.987 ml |
| 10 mM | 0.199 ml | 0.997 ml | 1.993 ml |
| 5 mM | 0.04 ml | 0.199 ml | 0.399 ml |
Last Update：2024-01-02 23:10:35
PHA-680632 - Reference Information
| biological activity | PHA-680632 is A potent inhibitor of Aurora A,Aurora B, and Aurora C with an IC50 of 27 nM, 135 nM and 120 nM, IC50 values 10 to 200 times higher than those for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3. PHA-680632 is A potent inhibitor of Aurora A,Aurora B, and Aurora C with IC50 of 27 nM, 135 nM, and 120 nM, respectively, compared to FGFR1, FLT3, LCK, PLK1, the IC50 values for STLK2, and VEGFR2/3 are 10 to 200-fold higher. |
| signature | PHA-680632 is a potent Aurora kinase selective inhibitor. |
| Target | Value |
| Aurora A | 27 nM |
| Aurora C | 120 nM |
| Aurora B | 135 nM |
| FGFR1 | 390 nM |
| PLK1 | 780 nM |
Last Update：2024-04-10 22:29:15
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CAS: 398493-79-3
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Product Name: PHA-680632 Visit Supplier Webpage Request for quotation
CAS: 398493-79-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 398493-79-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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