2. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. FLT3 Checkpoint Kinase (Chk)
  4. FLT3/CHK1-IN-2

FLT3/CHK1-IN-2 (Compound 30) 是 FLT3 和 CHK1 的双重抑制剂，对 CHK1、FLT3-WT 和 FLT-D835Y IC50 分别为 25.63、16.39、22.80 nM。FLT3/CHK1-IN-2 具有良好的口服 PK 特性和激酶选择性。FLT3/CHK1-IN-2可用于急性髓系白血病 (AML) 的研究。

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FLT3/CHK1-IN-2 Chemical Structure

FLT3/CHK1-IN-2 Chemical Structure

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FLT3/CHK1-IN-2 相关抗体

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查看 Checkpoint Kinase (Chk) 亚型特异性产品:

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Chk1 Chk2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML)[1].

体外研究
(In Vitro)

FLT3/CHK1-IN-2 对 MV4-11 细胞具有抗增殖活性 (IC50: <4 nM)[1]。
FLT3/CHK1-IN-2 对具有多种 FLT3 突变的 BaF3 细胞显示出抗增殖活性 (IC50: 对BaF3-FLT3-F691L、BaF3-FLT3 , D835F、BaF3-FLT3-D835V、BaF3-FLT3-ITD、BaF3-FLT3-ITD/D835Y 分别为 28.96、29.30、26.37、30.24、75.81 nM)[1]。
FLT3/CHK1-IN-2 (0-100 nM) 抑制 MV4-11 细胞中 FLT3 及其主要下游效应子 STAT5 (Tyr694)、AKT (Ser473) 和 ERK (Tyr204) 的磷酸化，并降低 pS296-CHK1 水平和 c-Myc 蛋白表达水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

FLT3/CHK1-IN-2 相关抗体:
体内研究
(In Vivo)

FLT3/CHK1-IN-2 (20 mg/kg，口服) 具有良好的 PK 特性，Cmax 为 2213.07 ng/mL，AUC(0−t) 为 2736.58 h·ng /mL[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

444.47

Formula

C18H23F3N6O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

FLT3/CHK1-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FLT3/CHK1-IN-2FLT3Checkpoint Kinase (Chk)Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3MV4-11 AMLInhibitorinhibitorinhibit

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