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NMS-P715 {[allProObj[0].p_purity_real_show]}

货号:A223438 Ambeed 开学季,买赠积分,赢豪礼

NMS-P715 is the first selective, ATP-competitive and orally bioavailable MPS1 small-molecule inhibitor (IC50=8 nM) and selectively reduces cancer cell proliferation, leaving normal cells almost unaffected.

NMS-P715 化学结构 CAS号:1202055-32-0
NMS-P715 化学结构
CAS号:1202055-32-0
NMS-P715 3D分子结构
CAS号:1202055-32-0
NMS-P715 化学结构 CAS号:1202055-32-0
NMS-P715 3D分子结构 CAS号:1202055-32-0
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NMS-P715 纯度/质量文件 产品仅供科研

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NMS-P715 生物活性

描述 NMS-P715 is a selective MPS1 inhibitor with an IC50 of 182 nM. It is highly specific, affecting no kinases below a 5 μM IC50 and only inhibiting CK2, MELK, and NEK6 under 10 μM. NMS-P715 triggers a significant spindle assembly checkpoint (SAC) bypass with an EC50 of 65 nM. At 1 μM, it accelerates mitosis in U2OS cells expressing YFP-α-tubulin, leads to aneuploidy, and suppresses HCT116 cell proliferation. Additionally, NMS-P715 (0.5, 1 μM) impacts the stability of the mitotic checkpoint complex (MCC) and cdc20 ubiquitination[1]. NMS-P715 (1 μM) enables spindle assembly checkpoint bypass and induces apoptosis in pancreatic ductal adenocarcinoma (PDAC) cell lines. Additionally, NMS-P715 (0-25 μM) selectively curtails the growth of PDAC cells[2].
体内研究

NMS-P715 (10 mg/kg) demonstrates 37% oral bioavailability and favorable pharmacokinetics in nude mice with human tumor cell xenografts implanted subcutaneously. At a dose of 90 mg/kg orally, NMS-P715 is well tolerated without causing body weight loss or noticeable toxicities in an A2780 ovarian carcinoma xenograft model. Furthermore, NMS-P715 (100 mg/kg, orally) reduces tumor growth by approximately 43% in the A375 melanoma xenograft model[1].

体外研究

NMS-P715 is a selective MPS1 inhibitor with an IC50 of 182 nM. It is highly specific, affecting no kinases below a 5 μM IC50 and only inhibiting CK2, MELK, and NEK6 under 10 μM. NMS-P715 triggers a significant spindle assembly checkpoint (SAC) bypass with an EC50 of 65 nM. At 1 μM, it accelerates mitosis in U2OS cells expressing YFP-α-tubulin, leads to aneuploidy, and suppresses HCT116 cell proliferation. Additionally, NMS-P715 (0.5, 1 μM) impacts the stability of the mitotic checkpoint complex (MCC) and cdc20 ubiquitination[1].

NMS-P715 (1 μM) enables spindle assembly checkpoint bypass and induces apoptosis in pancreatic ductal adenocarcinoma (PDAC) cell lines. Additionally, NMS-P715 (0-25 μM) selectively curtails the growth of PDAC cells[2].

NMS-P715 参考文献

[1]Colombo R, et al. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res. 2010 Dec 15;70(24):10255-64.

[2]Slee RB, et al. Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor NMS-P715. Mol Cancer Ther. 2014 Feb;13(2):307-315.

NMS-P715 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.48mL

0.30mL

0.15mL

7.39mL

1.48mL

0.74mL

14.78mL

2.96mL

1.48mL

NMS-P715 技术信息

CAS号1202055-32-0
分子式C35H39F3N8O3
分子量 676.731
别名
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 2 mg/mL(2.96 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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