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

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 BUBR1

  • 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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
26.37 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
BaF3 IC50
28.96 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
BaF3 IC50
29.3 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835F mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835F mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
BaF3 IC50
30.24 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
BaF3 IC50
75.81 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
MV4-11 IC50
2.96 nM
Compound: 30
Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
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

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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)
× = ×
C1   V1   C2   V2
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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