2. Protein Tyrosine Kinase/RTK Apoptosis JAK/STAT Signaling Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR
  3. FLT3 Apoptosis STAT p38 MAPK Akt
  4. FLT3-IN-32 hydrochloride

FLT3-IN-32 hydrochloride 是一种强效且口服有效的 FLT3 抑制剂，其针对 FLT3-ITD、FLT3-D835Y 和 FLT-N676K 的 IC50 值分别为 0.29 nM、0.77 nM 和 2.07 nM。FLT3-IN-32 hydrochloride 通过降低 FLT3及其下游信号分子 (STAT5、MAPK、AKT) 的磷酸化，诱导 FLT3 突变 Ba/F3 细胞凋亡 (apoptosis)。FLT3-IN-32 hydrochloride在 MV4-11异种移植模型中具备强大的抗肿瘤效果。FLT3-IN-32 hydrochloride 可用于急性髓性白血病 (AML) 的研究。

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FLT3-IN-32 hydrochloride

FLT3-IN-32 hydrochloride Chemical Structure

CAS No. : 3047195-66-1

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Other Forms of FLT3-IN-32 hydrochloride:

FLT3-IN-32 hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 STAT 亚型特异性产品:

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STAT3 STAT5 STAT6 STAT1

查看 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FLT3-IN-32 hydrochloride is a potent and orally active FLT3 inhibitor with an IC50s of 0.29 nM, 0.77 nM and 2.07 nM against FLT3-ITD, FLT3-D835Y and FLT-N676K. FLT3-IN-32 hydrochloride reduces the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT) to induce FLT3-mutated Ba/F3 cells apoptosis. FLT3-IN-32 hydrochloride shows significant anti-tumor efficacy in n the MV4-11 xenograft model. FLT3-IN-32 hydrochloride can be used for the study of acute myeloid leukemia (AML)[1].

IC50 & Target[1]

STAT5

 

Akt

 

体外研究
(In Vitro)

FLT3-IN-32 hydrochloride (Compound 29c) (0-100 nM, 72 h) 对肝细胞 HepG2、肺癌细胞 NCI-H460 和内皮细胞 HMEC-1 无细胞毒性，仅特异性抑制表达不同 FLT3 抗性的 Ba/F3 pMIY 细胞 (ITD-突变 NPOS，TKD-突变 D835Y，ITD-突变 NPOS 和 TKD-突变 D835Y，ITD-突变 NPOS 和 TKD-突变 N676K)[1]。
FLT3-IN-32 hydrochloride (1-500 nM, 4-48 h) 通过降低 FLT3 磷酸化诱导 Ba/F3 pMIY 细胞凋亡[1]。

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

FLT3-IN-32 hydrochloride 相关抗体:

Apoptosis Analysis[1]

Cell Line: Ba/F3 pMIY cells expressing different FLT3 resistance (ITD-Mutation NPOS, TKD-Mutation D835Y, ITD-Mutation NPOS and TKD-Mutation D835Y, ITD-Mutation NPOS and TKD-Mutation N676K)
Concentration: 5, 20, 100 and 500 nM
Incubation Time: 48 h
Result: Dose-dependently induced apoptosis in FLT3-mutated Ba/F3 cells, especially in D835Y and N676K drug-resistant mutants.

Western Blot Analysis[1]

Cell Line: Ba/F3 cells expressing FLT3-ITD(NPOS)
Concentration: 1, 5, 10, 20, 50 nM
Incubation Time: 4 h
Result: Concentration-dependently reduced the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT).
体内研究
(In Vivo)

20(R)-Ginsenoside Rh2 (20-75 mg/kg, p.o and i.p., 每日一次共 4-5 天) 在 MV4-11 异种移植小鼠模型中显示出抗肿瘤功效和良好的耐受性[1]。

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

Animal Model: MV4-11 xenograft model established in female NOD/SCID mice (6-8 weeks)[1]
Dosage: 50 mg/kg
Administration: Oral administration (p.o.), once daily for 5 days
Result: Effectively inhibited tumor growth and prolonged the survival of mice.
Animal Model: Tolerability study established in female NOD/SCID mice (6-8 weeks)[1]
Dosage: 20, 50, 75 mg/kg
Administration: Oral administration (p.o.) and intraperitoneal injection (i.p.) once daily for 4 days
Result: No drug-related deaths.
Experienced transient weight loss, which is recoverable, with no severe clinical symptoms at doses up to 75 mg/kg.
分子量

552.02

Formula

C28H30ClN5O5
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-IN-32 hydrochloride 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-IN-323047195-66-1FLT3ApoptosisSTATp38 MAPKAktCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3PKBProtein kinase BAcute myleoid leukemiaFLT3 mutationsIn vivo mouse modelType I/II inhibitorTyrosine kinase inhibitorInhibitorinhibitorinhibit

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