计算溶液所需的质量、体积或浓度。
概述
MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC 50 of 21 nM.
In Vitro
MI-538 inhibits the proliferation of MLL leukemia cells with a GI 50 of 83 nM. MI-538 shows no effect (up to 6 μM) on growth of the control cell lines HL-60 and HM-2, which do not harbor MLL translocations, demonstrating good selectivity toward MLL fusion protein transformed cells. MI-538 binds to menin with low nanomolar affinity (K d =6.5 nM). Its potent cellular activity originates from the improved binding affinity to menin and possibly increased cell membrane permeability. Treatment with MI-538 results in strong down regulation of expression of Hoxa9 and Meis1 genes. About 100 nM 27 was sufficient to reduce by ~50% Hoxa9 expression in MLL-AF9 cells, and even more pronounced effect was seen on Meis1 expression. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Treatment with MI-538 results in a pronounced, about 80%, reduction in the MV4;11 tumor volume, without causing substantial signs of toxicity reflected by less than 10% reduction of the body weight. MI-538 demonstrates markedly improved exposure (area under the curve, AUC, values), Cmax (maximum compound concentration) in the blood plasma, and the lowest value of clearance. The half-life of MI-538 is about 1.6 h. MI-538 has also high oral bioavailability (~50%) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:IC50 : 21 nM (menin and MLL interaction),Kd: 6.5 nM (menin)
规格
规格或纯度
≥98%
英文名称
MI-538
生化机理
MI-538 是 Menin 与 MLL 融合蛋白相互作用的抑制剂，其 IC 50 为 21 nM。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
566.60
高级数据
化学和物理性质
溶解性
DMSO : 100 mg/mL (176.49 mM; Need ultrasonic)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥98%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C条件下保存。需冷冻保存以维持规定的有效期。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1857417-10-7，分子式为 C27H25F3N8OS，分子量为 566.60 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
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危险品化学品经营许可证（带存储）