| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| I408530-1ml |
1ml |
期货  |
|
| 别名 | 伊沙佐米 (MLN2238) |
|---|---|
| 英文别名 | (R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutylboronic acid |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Ixazomib (MLN2238) |
| 生化机理 | 伊沙佐米（MLN2238）可抑制 20S 蛋白酶体的糜蛋白酶样蛋白水解位点（β5），在无细胞实验中的 IC50 和Ki分别为 3.4 nM 和 0.93 nM，还可抑制类 Caspase（β1）和类胰蛋白酶（β2）蛋白水解位点，IC50 分别为 31 nM 和 3500 nM。伊沙佐米（MLN2238）可诱导自噬。第 3 阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 26S 蛋白酶体抑制剂 |
| 产品介绍 |
MLN2238(Ixazomib)能抑制20S蛋白酶体的糜蛋白酶样蛋白水解位点(β5)，IC50和Ki分别为3.4 nM和0.93 nM。 Information Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the20S proteasomewithIC50andKiof 3.4 nM and 0.93 nM in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 At higher concentrations, MLN2238 also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31nM and 3.5uM, respectively. MLN2238 inhibits Calu-6 cell with IC50 of 9.7 nM. MLN2238 is a selective, potent, and reversible inhibitor of the proteasome in tumor cells. MLN2238 shows time-dependent reversible proteasome inhibition. Both MLN2238 and Bortezomib shows time-dependent reversible proteasome inhibition; however, the proteasome dissociation half-life for MLN2238 is determined to be ∼6-fold faster than that of Bortezomib (18 and 110 minutes, respectively). MLN2238 dissociates more rapidly from the proteasome than Bortezomib, consistent with faster recovery of proteasome activity observed in the Proteasome-Glo assay. MLN2238 has a greater overall tumor pharmacodynamic effect than Bortezomib as assessed by 20S inhibition. MLN2238 is the biologically active form of MLN9708. In vivo MLN2238 induces a greater pharmacodynamic response than Bortezomib in xenograft tumors. MLN2238 shows greater maximum and sustained tumor proteasome inhibition compared with Bortezomib in xenograft models. These results confirm that the improved tumor exposure seen with MLN2238 translates into an improved tumor pharmacodynamic response both at the level of and downstream from the proteasome. MLN2238 shows antitumor activity in the CWR22 xenograft model. MLN2238 shows greater tumor pharmacodynamic responses in WSU-DLCL2 xenografts compared with Bortezomib. Similarly, Bortezomib treatment only led to a minor increase in GADD34 levels in WSU-DLCL2 xenograft tumors, whereas MLN2238 strongly induces its expression. MLN2238 has an improved pharmacodynamic profile and antitumor activity compared with Bortezomib in both OCI-Ly10 and PHTX22L models. cell lines： Concentrations：~10 nM Incubation Time：1 hour or 30 minutes Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | B([C@H](CC(C)C)NC(=O)CNC(=O)C1=C(C=CC(=C1)Cl)Cl)(O)O |
| 分子量 | 361.03 |
| Reaxy-Rn | 31323510 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=31323510&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 28 mg/mL (202.64 mM); Water: 28 mg/mL (202.64 mM); Ethanol: 28 mg/mL (202.64 mM); |
|---|
| 象形图 | GHS08 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H360: 可能损害生育力或未出生的孩子 H362: 可能对母乳喂养的孩子造成伤害 |
| 预防措施声明 |
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P263: 避免在怀孕期间/哺乳期间接触。 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。 |
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