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- 详细信息
- 技术资料
- 库存:
33
- 英文名:
CPI-1205
- CAS号:
1621862-70-1
- 供应商:
上海莼试
- 保存条件:
Store at -20°C
- 规格:
2mg 5mg 25mg
使用方法:
1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性:
产品描述:
分子式:C27H33F3N4O3

分子量:518.57
溶解度:Soluble in DMSO
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
0.002 μM for biochemical IC50; 0.032 μM for cellular EC50.CPI-1205 is an EZH2 inhibitor.Polycomb repressive complex 2 (PRC2) plays a key role in transcriptional silencing partially by installing methylation marks on lysine 27 of histone 3. Dysregulation of PRC2 function relates with certain malignancies and poor prognosis. EZH2 is thus representing a promising candidate oncology target for pharmacological intervention.In vitro: Previous study reported that the treatment with CPI-1205 caused apoptosis in multiple myeloma and plasmacytoma cell models. CPI-1205 also had a clean selectivity profile when tested against 30 other histone or DNA methyltransferases. In addition, CPI-1205 demonstrated modest selectivity when tested against enhancer of zeste homologue 1 (EZH1) that is a methyltransferase highly related to EZH2 [1].In vivo: In animal study, CPI-1205 was dosed at 160 mg/kg orally twice daily for 25 days in tumor bearing female CB-17 SCID mice. By the treatment of tumor-bearing mice with CPI-1205, tumor regression was orved within two weeks. By the end of day 25, significant tumor growth inhibition was recorded. CPI-1205 was found to be well-tolerated for repeat dosing as orved by the ance of significant body weight loss. In addition, analysis of plasma and tumor at 1 h post last dose on day 25 showed sufficient plasma and tumor tissue concentrations [1].Clinical trial: A study to evaluate CPI-1205 in patients with B-cell lymphomas is currently recruiting participants [2].
注意事项:
抗逆滴加序列
每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
反应时间及温度
加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
公司正在出售的产品:
1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性:
| 货号 | CS-01Y67328 | 规格 | 2mg 5mg 25mg |
| CAS号 | 1621862-70-1 | 分子量 | 518.57 |
| 含量 | >98.00% | 别名 | |
| 分子式 | C27H33F3N4O3 | 化学名 | (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C27H33F3N4O3

分子量:518.57
溶解度:Soluble in DMSO
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
0.002 μM for biochemical IC50; 0.032 μM for cellular EC50.CPI-1205 is an EZH2 inhibitor.Polycomb repressive complex 2 (PRC2) plays a key role in transcriptional silencing partially by installing methylation marks on lysine 27 of histone 3. Dysregulation of PRC2 function relates with certain malignancies and poor prognosis. EZH2 is thus representing a promising candidate oncology target for pharmacological intervention.In vitro: Previous study reported that the treatment with CPI-1205 caused apoptosis in multiple myeloma and plasmacytoma cell models. CPI-1205 also had a clean selectivity profile when tested against 30 other histone or DNA methyltransferases. In addition, CPI-1205 demonstrated modest selectivity when tested against enhancer of zeste homologue 1 (EZH1) that is a methyltransferase highly related to EZH2 [1].In vivo: In animal study, CPI-1205 was dosed at 160 mg/kg orally twice daily for 25 days in tumor bearing female CB-17 SCID mice. By the treatment of tumor-bearing mice with CPI-1205, tumor regression was orved within two weeks. By the end of day 25, significant tumor growth inhibition was recorded. CPI-1205 was found to be well-tolerated for repeat dosing as orved by the ance of significant body weight loss. In addition, analysis of plasma and tumor at 1 h post last dose on day 25 showed sufficient plasma and tumor tissue concentrations [1].Clinical trial: A study to evaluate CPI-1205 in patients with B-cell lymphomas is currently recruiting participants [2].
注意事项:
抗逆滴加序列
每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
反应时间及温度
加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
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CPI-1205
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