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CCT251455 Sale

目录号 : GC33213

CCT251455是有效和选择性的有丝分裂激酶单极纺锤体1(MPS1)抑制剂,IC50值为3nM。

CCT251455 Chemical Structure

Cas No.:1400284-80-1

规格 价格 库存 购买数量
250mg 待询 待询
500mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

HCT116 cells are treated with 0-20 μM CCT251455 for 72 h. Cell viability is measured using the MTT assay[1].

Animal experiment:

Mice[1][1]Human HCT116 colon carcinoma cells are sc injected bilaterally in the flanks of female CrTac:NCr-Fox1(nu) athymic mice. Once tumors reach a mean diameter of 8 mm (day 15), mice are dosed twice at a 12 h intervals with 50, 75, or 100 mg/kg of CCT251455 in 10% (v/v) DMSO and 5% (v/v) Tween 20 in saline. Mice are culled (n=3 per group) at 2, 10, and 72 h after the second dose. Tumors are snap-frozen and stored at -80 °C until analysis[1].

References:

[1]. Naud S, et al. Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). J Med Chem. 2013 Dec 27;56(24):10045-65.

产品描述

CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC50 of 3 nM.

CCT251455 is a highly potent inhibitor of MPS1 that demonstrates high selectivity versus kinases tested in a broad kinome profiling panel. CCT251455 inhibits P-MPS1 with an IC50 of 0.04 μM in cell-based assay and has a GI50 of 0.16 μM[1].

CCT251455 demonstrates a good oral pharmacokinetic profile in mouse and rat as well as inhibition of MPS1 activity in vivo following oral administration[1].

[1]. Naud S, et al. Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). J Med Chem. 2013 Dec 27;56(24):10045-65.

Chemical Properties

Cas No. 1400284-80-1 SDF
Canonical SMILES O=C(N1C(C2=CN(C)N=C2)=CC3=C1C=C(NC4=CC=C(C5=CN=CN5C)C=C4Cl)N=C3)OC(C)(C)C
分子式 C26H26ClN7O2 分子量 503.98
溶解度 Soluble in DMSO 储存条件 Store at -20°C
General tips 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。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9842 mL 9.921 mL 19.8421 mL
5 mM 0.3968 mL 1.9842 mL 3.9684 mL
10 mM 0.1984 mL 0.9921 mL 1.9842 mL
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