CCT251455
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。
Cas No.:1400284-80-1
Sample solution is provided at 25 µL, 10mM.
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.
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. |
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。 |
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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。 |
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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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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