Ilorasertib
| CAS号 | 1227939-82-3 | 货号 | BCP07256 |
| 中文名 | Ilorasertib | ||
| 英文名 | Ilorasertib | ||
| 中文别名 | |||
| 英文别名 | ABT348;ABT 348; Abbott 968660; ABT-348; | ||
| 分子式 | C25H21FN6O2S | 分子量 | 488.54 |
| 生物活性 | ABT-348, is a novel potent and orally bioavailable inhibitor of the Aurora kinases as well as the VEGF and PDGF families of receptor tyrosine kinases and is currently in Phase I clinical trials. ABT-348 is is an ATP-competitive multitargeted kinase inhibitor with IC50s for inhibiting binding Aurora B (7 nM), C (1 nM), and A (120 nM), and also inhibits RET tyrosine kinase, PDGFRβ, and Flt1 with IC50s of 7 nM, 3 nM and 32 nM.ABT-348 has nanomolar potency (IC50) for inhibiting binding and cellular auto-phosphorylation of Aurora B (7 and 13 nM), C (1 and 13 nM) and A (120 and 189 nM). Based upon its unique spectrum of activity, ABT 348 was evaluated and found effective in representative solid tumor (HT1080 and MiaPaCa, tumor stasis) and hematological malignancy (RS4;11, regression) xenografts. These results provide the rationale for clinical assessment of ABT-348 as a therapeutic agent in the treatment of cancer. | ||
| 上下游产品 | 1847485-91-9（Ilorasertib hydrochloride ） | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase Cell Cycle/DNA Damage Epigenetics | ||
| 靶 点 | Aurora PDGFR VEGFR | ||
结构式
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