CAS NO: | 398493-79-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | PHA-680632 is anaurorakinase inhibitor withIC50s of 27, 135 and 120 nM foraurora A, B and C, respectively. | ||||||||||||||||
IC50& Target |
| ||||||||||||||||
体外研究 (In Vitro) | PHA-680632 shows 30- to 200-fold higherIC50s of FLT3, LCK, PLK1, STLK2, VEGFR2, and VEGFR3 compared with Aurora A. PHA-680632 has potent antiproliferative activity in a wide range of cell types. The IC50s are 0.32, 0.41, 0.06, 1.17, 0.56, 0.62, 0.29, 0.11, 1.56, 0.62, 0.07, 0.13, 0.41 μM for C33A, HeLa, HCT116, HT29, LOVO, A549, MCF7, A2780, U2OS, DU145, U937, HL60, NHDF. PHA-680632 can cause polyploidy in tumor cells. PHA-680632 cell treatment induces phenotypes similar to Aurora A or B depletion[1]. PHA680632, inhibits colony formation in different cancer cell lines and induced polyploidy. Aurora-A inhibition by PHA680632 enhances radiation response in cancer cells, especially in p53-deficient cells[2]. | ||||||||||||||||
体内研究 (In Vivo) | PHA-680632 suppresses tumor growth in animal models. PHA-680632 treatment at 45 mg/kg dose results in 85% of TGI without signs of toxicity in the HL60 human acute myelogenous leukemia xenograft model. PHA-680632 treatment at 60 mg/kg i.v. b.i.d. for 5 days results in 78% of TGI without signs of toxicity in the A2780 human ovarian carcinoma model[1]. PHA680632 in association with radiation leads to an additive effect in cancer cells, especially in the p53-deficient cells, but does not act as a radiosensitiser[2]. | ||||||||||||||||
分子量 | 501.62 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C28H35N7O2 | ||||||||||||||||
CAS 号 | 398493-79-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
| ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 30 mg/mL(59.81 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
|