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- 上海莼试
- CS-01Y66993
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- 详细信息
- 技术资料
- 库存：
31
- 英文名：
CRA-026440
- CAS号：
847460-34-8
- 供应商：
上海莼试
- 保存条件：
Store at -20°C
- 规格：
1mg 5mg 10mg 20mg
商品属性：
产品描述：
分子式:C23H24N4O4
分子量:420.46
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
CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively.CRA-026440 inhibits pure recombinant isozymes HDAC1, HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the nanomolar range. Treatment of cultured tumor cell lines grown in vitro with CRA-026440 results in the accumulation of acetylated histone and acetylated tubulin, leading to an inhibition of tumor cell growth and the induction of apoptosis. To determine if HDAC inhibition by CRA-026440 affects the proliferation of tumor cells, a panel of human tumor cell lines is treated in vitro at various concentrations of inhibitor. Antitumor activity is orved in all 10 tumor cell lines tested, with GI50 values ranging from 0.12 to 9.95 μM. In addition, CRA-026440 has antiproliferative effect on HUVEC endothelial cells with a GI50 value of 1.41 μM[1].CRA-026440 parenterally given to mice harboring HCT116 or U937 human tumor xenografts results in a statistically significant reduction in tumor growth. CRA-026440 is delivered i.v. to mice, and plasma concentrations are monitored over time. Based on these data, the clearance is calculated to be 38 mL/min/kg; the volume of distribution in the central compartment is 67 mL/kg. The steady-state volume of distribution is 454 mL/kg. The predominant plasma half-life is 7 minutes (44% of area under the curve); and the mean residence time is 12 minutes. One notable finding is that CRA-026440 has a different pharmacokinetic profile in tumor. It has a lower Cmax, but the compound concentration is maintained more steadily over time, probably due to the compound's large volume of distribution. CRA-026440 at 25 and 50 mg/kg given qdx3 per week significantly inhibits tumor growth at 40% (P<0.01) and 58% (P<0.01), respectively. The combination of Avastin at 25 mg/kg once a week and CRA-026440 at 25 and 50 mg/kg for three consecutive days per week lead to more profound tumor growth inhibition of 84% (P< 0.01) and 85% (P<0.01), respectively. Compared with Avastin alone, the combination yields a marginally better result (P<0.1). The combination of Avastin and CRA-026440 at 50 mg/kg is significantly better than CRA-026440 alone at 50 mg/kg (P<0.05). Both combination treatments are well tolerated with maximal weight loss <3%[1].[1]. Cao ZA, et al. CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo. Mol Cancer Ther. 2006 Jul;5(7):1693-701.
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。
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。
公司正在出售的产品：
| 货号 | CS-01Y66993 | 规格 | 1mg 5mg 10mg 20mg |
| CAS号 | 847460-34-8 | 分子量 | 420.46 |
| 含量 | >98.00% | 别名 | N/A |
| 分子式 | C23H24N4O4 | 化学名 | N/A |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C23H24N4O4
分子量:420.46
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
CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively.CRA-026440 inhibits pure recombinant isozymes HDAC1, HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the nanomolar range. Treatment of cultured tumor cell lines grown in vitro with CRA-026440 results in the accumulation of acetylated histone and acetylated tubulin, leading to an inhibition of tumor cell growth and the induction of apoptosis. To determine if HDAC inhibition by CRA-026440 affects the proliferation of tumor cells, a panel of human tumor cell lines is treated in vitro at various concentrations of inhibitor. Antitumor activity is orved in all 10 tumor cell lines tested, with GI50 values ranging from 0.12 to 9.95 μM. In addition, CRA-026440 has antiproliferative effect on HUVEC endothelial cells with a GI50 value of 1.41 μM[1].CRA-026440 parenterally given to mice harboring HCT116 or U937 human tumor xenografts results in a statistically significant reduction in tumor growth. CRA-026440 is delivered i.v. to mice, and plasma concentrations are monitored over time. Based on these data, the clearance is calculated to be 38 mL/min/kg; the volume of distribution in the central compartment is 67 mL/kg. The steady-state volume of distribution is 454 mL/kg. The predominant plasma half-life is 7 minutes (44% of area under the curve); and the mean residence time is 12 minutes. One notable finding is that CRA-026440 has a different pharmacokinetic profile in tumor. It has a lower Cmax, but the compound concentration is maintained more steadily over time, probably due to the compound's large volume of distribution. CRA-026440 at 25 and 50 mg/kg given qdx3 per week significantly inhibits tumor growth at 40% (P<0.01) and 58% (P<0.01), respectively. The combination of Avastin at 25 mg/kg once a week and CRA-026440 at 25 and 50 mg/kg for three consecutive days per week lead to more profound tumor growth inhibition of 84% (P< 0.01) and 85% (P<0.01), respectively. Compared with Avastin alone, the combination yields a marginally better result (P<0.1). The combination of Avastin and CRA-026440 at 50 mg/kg is significantly better than CRA-026440 alone at 50 mg/kg (P<0.05). Both combination treatments are well tolerated with maximal weight loss <3%[1].[1]. Cao ZA, et al. CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo. Mol Cancer Ther. 2006 Jul;5(7):1693-701.
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。
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。
公司正在出售的产品：
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CRA-026440
￥600 - 3200
