2. Protein Tyrosine Kinase/RTK
  3. FLT3
  4. FLT3/D835Y-IN-1

FLT3/D835Y-IN-1 (化合物13a) 是一种口服有效且选择性的 FLT3 和FLT3/D835Y 抑制剂，其 IC50 值分别为 0.26 nM 和 0.18 nM。FLT3/D835Y-IN-1 还能阻断肿瘤生长，具有抗癌作用，可以用于研究急性髓系白血病。

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FLT3/D835Y-IN-1 Chemical Structure

FLT3/D835Y-IN-1 Chemical Structure

CAS No. : 2648799-49-7

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FLT3/D835Y-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia)[1].

IC50 & TargetFLT3/D835Y

FLT3/D835Y

0.18 nM (IC50)

体外研究
(In Vitro)

FLT3/D835Y-IN-1 (compound 13a) (100 nM, 3 h) potently inhibits Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L cell lines, and AML cells proliferation[1].
FLT3/D835Y-IN-1 (3-30 nM, 16 h) significantly inhibit FLT3, AKT, ERK, and STAT5 pathways[1].

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

FLT3/D835Y-IN-1 相关抗体:

Cell Proliferation Assay

Cell Line: Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, and Ba/F3-FLT3-ITD-F691L cell lines, AML cells[1]
Concentration: 100 nM
Incubation Time: 3 h
Result: Inhibited Ba/F3-FLT3-ITD, Ba/F3-FLT3-ITD/D835Y, Ba/F3-FLT3-ITD-F691L, MV4-11, MOLM14, and MOLM14-ITD/D835Y proliferation, with GI50 values of 0.59, 0.73, 5.54, 1.30, 6.20, and 4.58 nM, respectively.

Western Blot Analysis

Cell Line: MOLM14-ITD/D835Y and MOLM14-ITD/F691L cells[1].
Concentration: 3, 10, and 30 nM
Incubation Time: 16 h
Result: Significantly inhibited the FLT3, AKT, ERK, and STAT5 pathways at lower dosages.
体内研究
(In Vivo)

FLT3/D835Y-IN-1 (10 mg/kg, IP, daily, 6 days per week) significantly suppresses tumor growth and exhibits potent antitumor activity against MOLM14-ITD/D835Y cells[1].
FLT3/D835Y-IN-1 (10 mg/kg, IV or Orally, single) displays extremely low AUC and high clearance[1].
Pharmacokinetic Parameters of FLT3/D835Y-IN-1 in ICR mice[1].

Parameters 13a
AUClast (ng*h/mL) 1360 ± 110
CL (L/h/kg) 6.96 ± 0.66
Vss (L/kg) 14.8 ± 0.7
T1/2 (h) 1.5 ± 0.1

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

Animal Model: NOD/SCID mice (6 weeks, male, nine mice per group)[1]
Dosage: 10 mg/kg
Administration: IP, daily, 6 days per week, from day 7 to day 29
Result: Significantly suppressed tumor growth.
Animal Model: ICR mice (7–8 weeks, male)[1]
Dosage: 10 mg/kg, dissolved in a solution (10% DMSO, 40% PEG400, and 50% PBS)
Administration: IV or Orally, single (Pharmacokinetic Analysis)
Result: Displayed extremely low AUC and high clearance.
分子量

403.43

Formula

C22H21N5O3
CAS 号
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/D835Y-IN-1 相关分类

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  • 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/D835Y-IN-12648799-49-7FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3MOLM-14 cellsSecondary mutationAcute myeloid leukemiaPharmacokinetic propertiesICR miceNOD/SCID miceDownstream signaling pathwayInhibitorinhibitorinhibit

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