| Bioactivity | Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s of <100 nM and 120 nM, respectively[1][2][3]. | ||||||||||||
| Invitro | Padnarsertib 可减弱 PAK4/β-catenin通 路，导致 NAD 耗损，并可减弱几种 RCC 细胞系的活力、侵袭和迁移。在无细胞酶分析中，利用重组 NAMPT 对 NAMPT 的抑制表明，Padnarsertib 的 IC50 约为 120 nM。Padnarsertib 可减弱 G2-M 转运并诱导 RCC 细胞株凋亡[2]。 | ||||||||||||
| In Vivo | Padnarsertib 显示出与 Sunitinib (HY-10255A) 相当的减少异种移植物生长的效力。Padnarsertib 对正常人 RPTEC 的影响很小，在体内没有明显的毒性[2]。Padnarsertib (口服；100 mg/kg 或 200 mg/kg；一天两次；共 14 天) 导致动物模型中异种移植物生长下降，且不显著影响动物体重。8 小时后，实验结束时，测定小鼠血浆和肿瘤中的浓度分别为 10757 ng/mL 和 10647 ng/mL[3]。 Animal Model: | ||||||||||||
| Name | Padnarsertib | ||||||||||||
| CAS | 1643913-93-2 | ||||||||||||
| Formula | C35H29F3N4O3 | ||||||||||||
| Molar Mass | 610.63 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. WO2015003166A1 [2]. Abu Aboud O, et al. Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth. Mol Cancer Ther. 2016 Sep;15(9):2119-29. [3]. Abu Aboud O, et al. Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth.Mol Cancer Ther. 2016 Sep;15(9):2119-29. |
Padnarsertib
CAS: 1643913-93-2 F: C35H29F3N4O3 W: 610.63
Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, w
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