标签归档：itd

FLT3/ITD-IN-2

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FLT3/ITD-IN-2 

FLT3/ITD-IN-2 (Compound 17) 是一种有效的 FLT3-ITD 抑制剂，对 FLT3D835Y、FLT3 和 FLT3-ITD 的 IC50 值分别为 0.3、0.4 和 1.0 nM。FLT3/ITD-IN-2 有效抑制 FLT3 的磷酸化，对急性髓系白血病细胞具有良好的抗增殖活性。

FLT3/ITD-IN-2

FLT3/ITD-IN-2 Chemical Structure

CAS No. : 2489446-59-3

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生物活性

FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines[1].

IC50 & Target

IC50: 0.3 nM (FLT3D835Y), 0.4 nM (FLT3), 1.0 nM (FLT3-ITD)[1]
分子量

489.49

Formula

C23H26F3N7O2
CAS 号

2489446-59-3
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.
参考文献

  • [1]. Chen Y, et al. Discovery and structure – activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors. Bioorg Med Chem. 2021 Oct 15;48:116422.

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FLT3/ITD-IN-3

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FLT3/ITD-IN-3 

FLT3/ITD-IN-3 (Compound 19) 是一种有效的 FLT3-ITD 抑制剂，对 FLT3D835Y、FLT3 和 FLT3-ITD 的 IC50 值分别为 0.3、0.4 和 0.9 nM。FLT3/ITD-IN-3 有效抑制 FLT3 的磷酸化，对急性髓系白血病细胞具有良好的抗增殖活性。

FLT3/ITD-IN-3

FLT3/ITD-IN-3 Chemical Structure

CAS No. : 2489446-47-9

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生物活性

FLT3/ITD-IN-3 (Compound 19) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 0.9 nM against FLT3D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-3 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines[1].

IC50 & Target

IC50: 0.3 nM (FLT3D835Y), 0.4 nM (FLT3), 0.9 nM (FLT3-ITD)[1]
分子量

455.94

Formula

C22H26ClN7O2
CAS 号

2489446-47-9
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.
参考文献

  • [1]. Chen Y, et al. Discovery and structure – activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors. Bioorg Med Chem. 2021 Oct 15;48:116422.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

FLT3/ITD-IN-4

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FLT3/ITD-IN-4 

FLT3/ITD-IN-4 (Compound 16) 是一种选择性的 FLT3 内部串联重复突变 (FLT3-ITD) 抑制剂，IC50 值为 2.3 nM。FLT3/ITD-IN-4 可用于急性骨髓性白血病的研究。

FLT3/ITD-IN-4

FLT3/ITD-IN-4 Chemical Structure

CAS No. : 2278278-04-7

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生物活性

FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC50 of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research[1].

IC50 & Target

CDK16/Cyclin Y

1768 nM (EC50)

MAP4K4

5737 nM (EC50)

FLT3-ITD

2.3 nM (IC50)

FLT3 D835Y

4.84 nM (IC50)

RET

277 nM (EC50)

FLT3

443 nM (EC50)

ZAK/MLTK

1069 nM (EC50)

DDR2

2494 nM (EC50)

EPHA7

3255 nM (EC50)

NTRK1

3857 nM (EC50)

分子量

458.47

Formula

C25H22N4O5
CAS 号

2278278-04-7
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.
参考文献

  • [1]. Sellmer A, et al. A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia. Eur J Med Chem. 2020 May 1;193:112232.

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FLT3/ITD-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FLT3/ITD-IN-1 

FLT3/ITD-IN-1 (Compound 1) 是一种有效的 FLT3-ITD 抑制剂，对 FLT3 和 FLT3-ITD 的 IC50 值分别为 38.2 nM 和 144.1 nM。FLT3/ITD-IN-1 对急性髓系白血病细胞具有良好的抗增殖活性。

FLT3/ITD-IN-1

FLT3/ITD-IN-1 Chemical Structure

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生物活性

FLT3/ITD-IN-1 (Compound 1) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 38.2 nM and 144.1 nM against FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-1 displays excellent antiproliferative activities against acute myeloid leukemia cell lines[1].

IC50 & Target

IC50: 38.2 nM (FLT3), 144.1 nM (FLT3-ITD)[1]
分子量

366.42

Formula

C19H22N6O2
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.
参考文献

  • [1]. Chen Y, et al. Discovery and structure – activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors. Bioorg Med Chem. 2021 Oct 15;48:116422.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BSc5371

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BSc5371 

BSc5371 是一种有效的、不可逆的 FLT3 抑制剂，对 FLT3 突变体 FLT3(D835H)，FLT3(ITD, D835V)，FLT3(ITD, F691L)，FLT3-ITD 和野生型 FLT3wt 的 Kd 值分别为 1.3，0.83，1.5，5.8 和 2.3 nM。BSc5371 对 FLT3 依赖性的细胞具有细胞毒性。

BSc5371

BSc5371 Chemical Structure

CAS No. : 2286419-03-0

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生物活性

BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines[1].

IC50 & Target

Kd: 1.3 nM (LT3(D835H)), 0.83 nM (LT3(ITD, D835V)), 1.5 nM (LT3(ITD, F691L)), 5.8 nM (FLT3-ITD), 2.3 nM (FLT3wt)[1]
体外研究
(In Vitro)

BSc5371 (5 μM-0.5 nM, 77 hours) exhibits inhibitory activity against FLT3-mutated (MV4-11) cells, with an IC50 of 6 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 0.5 nM, 2.5 nM, 5 nM, 25 nM, 50 nM, 250 nM, 500 nM and 5 μM
Incubation Time: 77 hours
Result: Exhibited inhibitory activity against MV4-11 cells, with an IC50 of 6 nM.

分子量

485.60

Formula

C24H31N5O4S
CAS 号

2286419-03-0
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.
参考文献

  • [1]. Bensinger D, et al. Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. J Med Chem. 2019 Mar 14;62(5):2428-2446.

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