UNC5293
目录号: PL03274 纯度: ≥99%
CAS No. :2226789-82-6
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中文名称
UNC5293
英文名称
UNC5293
英文别名
UNC5293;Schembl21749867
Cas No.
2226789-82-6
分子式
C30H42N6O2
分子量
518.69
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
UNC5293 是一种 MERTK 选择性的有效抑制剂 (Ki=190 pM)。UNC5293 抑制 MERTK (IC50=0.9 nM),对 Axl、Tyro3 和 Flt3 更具选择性。UNC5293 表现出优异的小鼠药代动力学特性,并可以被用于骨髓白血病研究。
生物活性
UNC5293 is a MERTK-selective and potent inhibitor (K i =190 pM). UNC5293 inhibits MERTK (IC 50 =0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research.
性状
Viscous liquid
IC50 & Target[1][2]
Ki: 190 pM (MERTK)
IC50: 0.9 nM (MERTK)
体外研究(In Vitro)
UNC5293 provides selective target inhibition in cell-based assays. In cultures of the human B-cell acute lymphoblastic leukemia (B-ALL) cell line, UNC5293 inhibits phosphorylation of MERTK with an IC50 of 9.4 nM. In the SEM B-ALL cell line, UNC5293 is less potent against FLT3, with an IC50 of 170 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
UNC5293 (oral administration; 120 mg/kg; single dose) effectively inhibit MERTK in vivo in orthotopic 697 B-ALL mice xenografts.
UNC5293 (oral gavage; 3 mg/kg; single dose) has excellent mouse PK properties (7.8 h half-life and 58% oral bioavailability), and the C max and AUC last are 9.2 μM and 2.5 h*μM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Hongchao Zheng, et al. UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem. 2021 May 17;220:113534.
溶解度数据
In Vitro: DMSO : 100 mg/mL (192.79 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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