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- 详细信息
- 技术资料
- 库存:
56
- 英文名:
AG-221 (Enasidenib)
- CAS号:
1446502-11-9
- 供应商:
上海莼试
- 保存条件:
Store at -20°C
- 规格:
5mg 25mg 100mg
商品属性:
产品描述:
分子式:C19H17F6N7O
分子量:473.37
溶解度:-20°C
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
IC50: ~16 nM for IDH2 R140Q mutant
AG-221 (Enasidenib) is a mutant isocitrate dehydrogenase 2 (IDH2) inhibitor.
The somatic mutations of IDH1 and IDH2 are found in patients with acute myeloid leukemia. Leukemia-associated IDH1/2 mutations lead to aberrant accumulation of the oncometabolite 2-hydroxyglutarate (2-HG).
In vitro: AG-221 was found to be able to reduce 2-HG levels by >90%, reverse in-vitro histone and DNA hypermethylation, and induce differentiation in leukemia cell model as well. In addition, a dose dependent proliferative burst of the human specific CD45+ blast cells was oerved by the treatment of AG-221, as measured by the expression of CD11b, CD14, CD15 and cell morphology [1].
In vivo: The efficacy of AG-221 in a primary human AML xenograft model with the IDH2 R140Q mutation was studied, and the results showed that AG-221 could reduce 2-HG in the plasma, bone marrow, and urine of engrafted mice potently. In addition, the treatment of AG-221 could also induce a significant and dose dependent survival benefit as demonstrated by that all mice in the high dose treatment of AG-221 survived to the end of study [1].
Clinical trial: A phase 1, multicenter, dose-escalation, safety, PK, PD, and clinical activity study of AG-221 in patients with advanced hematologic malignancies with an IDH2 mutation has been conducted [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。
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-01Y63761 | 规格 | 5mg 25mg 100mg |
| CAS号 | 1446502-11-9 | 分子量 | 473.37 |
| 含量 | >95.00% | 别名 | 2-methyl-1-((4-(6-(trifluoromethyl)pyridin-2-yl)-6-((2-(trifluoromethyl)pyridin-4-yl)amino)-1,3,5-triazin-2-yl)amino)propan-2-ol |
| 分子式 | C19H17F6N7O | 化学名 | N/A |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C19H17F6N7O
分子量:473.37
溶解度:-20°C
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
IC50: ~16 nM for IDH2 R140Q mutant
AG-221 (Enasidenib) is a mutant isocitrate dehydrogenase 2 (IDH2) inhibitor.
The somatic mutations of IDH1 and IDH2 are found in patients with acute myeloid leukemia. Leukemia-associated IDH1/2 mutations lead to aberrant accumulation of the oncometabolite 2-hydroxyglutarate (2-HG).
In vitro: AG-221 was found to be able to reduce 2-HG levels by >90%, reverse in-vitro histone and DNA hypermethylation, and induce differentiation in leukemia cell model as well. In addition, a dose dependent proliferative burst of the human specific CD45+ blast cells was oerved by the treatment of AG-221, as measured by the expression of CD11b, CD14, CD15 and cell morphology [1].
In vivo: The efficacy of AG-221 in a primary human AML xenograft model with the IDH2 R140Q mutation was studied, and the results showed that AG-221 could reduce 2-HG in the plasma, bone marrow, and urine of engrafted mice potently. In addition, the treatment of AG-221 could also induce a significant and dose dependent survival benefit as demonstrated by that all mice in the high dose treatment of AG-221 survived to the end of study [1].
Clinical trial: A phase 1, multicenter, dose-escalation, safety, PK, PD, and clinical activity study of AG-221 in patients with advanced hematologic malignancies with an IDH2 mutation has been conducted [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。
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。
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AG-221 (Enasidenib)
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