Hesperadin hydrochloride 是Aurora A和B的 ATP 竞争性吲哚酮抑制剂。Hesperadin hydrochloride 以 250 nM 的IC50抑制 Aurora B。
| 生物活性 | Hesperadin hydrochloride is an ATP competitive indolinone inhibitor ofAurora AandB. Hesperadin hydrochloride inhibitsAurora Bwith anIC50of 250 nM[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | Hesperadin (10-100 nM) inhibits the Aurora kinase-1 (TbAUK1)-mediated phosphoryation of trypanosome histone H3 (TbH3) in a dose dependent manner, with an IC50of 40 nM[1].
Hesperadin (0.01-10 μM; 24 or 48 hours) inhibits growth of bloodstream forms (BF) and procyclic forms (PF) cultures[1].
Hesperadin (100-200 nM; 24-72 hours) alters cell morphology and inhibits cell cycle progression similar to the RNAi knockdown of TbAUK1[1].
Cell Viability Assay[1] | Cell Line: | M110 cells | | Concentration: | 0.01, 0.1, 1, 10 μM | | Incubation Time: | 24 hours or 48 hours | | Result: | Inhibiting growth of BF cultures with an IC50of 50 nM, while the inhibition of PF growth required approximately 11-fold more Hesperadin, with an IC50of 550 nM. |
Cell Cycle Analysis[1] | Cell Line: | M110 cells | | Concentration: | 100, 200 nM | | Incubation Time: | 24, 48, 72 hours | | Result: | Had a strong effect on cell growth and mitotic progression at 100-200 nM. |
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体内研究
(In Vivo) | Hesperadin (20 mg/kg/d; i.v.) prolongs the survival of xenograft mice via synergistic effect with Temozolomide (TMZ)[2].
| Animal Model: | 6-week-old female nude mice injected GBM cells[2] | | Dosage: | 20 mg/kg/d | | Administration: | I.v. injection | | Result: | Increased the survival of xenograft mice models. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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