2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FLT3 Apoptosis
  4. FLT3-IN-32

FLT3-IN-32 是一种强效的 FLT3 抑制剂。FLT3-IN-32 对 FLT3 具有高选择性，可有效抑制 FLT3 激活突变并诱导细胞凋亡 (apoptosis)。FLT3-IN-32 在无肿瘤小鼠中表现出良好的耐受性。FLT3-IN-32 在负荷 MV4-11 细胞的 NOD/SCID 小鼠中显示出卓越的抗肿瘤功效，能够显著延长小鼠的生存期。FLT3-IN-32 可用于急性髓系白血病的研究。

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FLT3-IN-32 Chemical Structure

FLT3-IN-32 Chemical Structure

CAS No. : 3047195-48-9

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FLT3-IN-32 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-IN-32 is a potent FLT3 inhibitor. FLT3-IN-32 shows high selectivity for FLT3 and efficiently inhibits FLT3-activating mutations and induces apoptosis. FLT3-IN-32 shows good tolerability in non-tumor bearing mice. FLT3-IN-32 demonstrates outstanding anti-tumor efficacy in MV4-11 bearing NOD/SCID mice, prolonging the survival noticeably. FLT3-IN-32 can be used for the research of acute myeloid leukemia[1].

体外研究
(In Vitro)

FLT3-IN-32 (Compound 29c) (0.3-218.7 nM, 72 h) 可有效抑制四种表达突变型 FLT3 亚型的 Ba/F3 细胞的增殖[1]。

FLT3-IN-32 shows promising (1 μM-1 M) 对 FLT3-ITD 阳性细胞显示出良好的选择性和安全性[1]。

FLT3-IN-32 (100-500 nM, 48 h) 可诱导四种表达突变型 FLT3 亚型的 Ba/F3 细胞发生凋亡[1]。

FLT3-IN-32 (1-50 nM, 4 h) 可降低 FLT3的磷酸化水平和其下游信号分子 (STAT5、MAPK) 的水平[1]。

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

FLT3-IN-32 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Ba/F3 pMIY FLT3-ITD (NPOS), Ba/F3 pMIY FLT3 D835Y, Ba/F3 pMIY FLT3 NPOS D835Y, Ba/F3 pMIY FLT3 NPOS N 676K cells
Concentration: 0.3-218.7 nM
Incubation Time: 72 h
Result: Showed effectively inhibition with IC50 values of 0.29 nM, 0.77 nM, 11.69 nM and 2.07nM, respectively.

Apoptosis Analysis[1]

Cell Line: Ba/F3 pMIY FLT3-ITD (NPOS), Ba/F3 pMIY FLT3 D835Y, Ba/F3 pMIY FLT3 NPOS D835Y, Ba/F3 pMIY FLT3 NPOS N 676K cells
Concentration: 5, 20, 100,and 500 nM
Incubation Time: 48 h
Result: Showed highly potent in inducing apoptotsis in FLT3 D835Y cells (54.11 %) and FLT3 NPOS N676K cells (38.43 %) at 100 nM.

Cell Proliferation Assay[1]

Cell Line: Ba/F3 pMIY FLT3-ITD (NPOS) cells
Concentration: 1, 5, 10, 20, and 50 nM
Incubation Time: 4 h
Result: Decreased the levels of phosphorylation of FLT3 and its downstream signaling molecules including STAT5, MAPK and to a lesser extent also AKT in a concentration-dependent manner.
体内研究
(In Vivo)

FLT3-IN-32 (Compound 29c) (20-75 mg/kg；口服；每天一次，持续5天) 在负荷 MV4-11 细胞的 NOD/SCID 小鼠中显示出卓越的抗肿瘤效果[1]。

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

Animal Model: MV4-11 CDX (cell-line derived xenograft) model in non-tumor bearing NOD/SCID mice (female, 8-9 weeks)[1]
Dosage: 50 mg/kg
Administration: Oral administration, daily for 5 days
Result: Showed less relative body weight loss compared to Quizartinib (HY-13001) and comparable with Midostaurin (HY-10230).
Showed similarly inhibitive activity as Quizartinib (HY-13001) and much more active than Midostaurin (HY-10230).
Animal Model: Non-tumor bearing NOD/SCID mice (female, 6-8 weeks)[1]
Dosage: 20, 50, 75 mg/kg
Administration: Oral administration, Intraperitoneal injection (20, 50 mg/kg), 15 days
Result: Showed good tolerability
分子量

515.56

Formula

C28H29N5O5
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 相关分类

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  • 稀释计算器

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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-323047195-48-9FLT3ApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Acute myeloid leukemiaFMS-like tyrosine kinase (FLT3)MV4-11 cellsInhibitorinhibitorinhibit

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目录号：
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