货号	规格	价格	上海	北京	珠海	重庆	武汉
S89217-5mg促销	98.10%	￥1700.00 ￥1360.00 S89217-5mg ￥1360.00 现货	6 6	-	-	-	-
S89217-10mg促销	98.10%	￥2720.00 ￥2170.00 S89217-10mg ￥2170.00 现货	5 5	-	-	-	-
S89217-25mg促销	98.10%	￥4930.00 ￥3940.00 S89217-25mg ￥3940.00 现货	5 5	-	-	-	-
S89217-100mg促销	≥98%	￥10900.00 ￥8720.00 S89217-100mg ￥8720.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.

靶点：

IC50: 13 nM (FLT3 WT), 8 nM (FLT3 D835Y);FLT

体外研究：

FLT3-IN-3 (Compound 7d) inhibits the proliferation of FLT3-ITD positive MV4-11 and MOLM-13 cell lines very effectively at low nanomolar concentrations (GI50 values 2 and 1 nM, respectively). FLT3-IN-3 (1 nM, 10nM, 100 nM, 1 μM and 10 μM; 72 hours) inhibits the Ba/F3 FLT3-ITD cells with the GI50 of 0.034±0.015 μM, and inhibits the parental Ba/F3 cells with the GI50 value of 1.136±0.389 μM. Concentrations as low as 1 nM are sufficient to block the autophosphorylation of the FLT3 receptor tyrosine kinase at three different tyrosine residues (589, 591, and 842). Moreover, this inhibition suppresses phosphorylation of several downstream targets of FLT3. Notably, FLT3-IN-3 (0.01, 0.1, 1, 10 and 100 nM; 1 hours) abolishes phosphorylation of STAT5 at Y694, which is a direct substrate of the oncogenic FLT3-ITD variant. The second pathway affected is the MAPK cascade: Two key components of this signaling pathway, ERK1/2 (T202/Y204) and MEK1/2 (S217/221), exhibit reduced phosphorylation upon treatment with FLT3-IN-3. FLT3-IN-3 also interfers with PI3K/AKT pathway which is confirmed by reduced phosphorylation of AKT at S473. Cell Proliferation Assay Cell Line: Murine Ba/F3 FLT3-ITD and parental Ba/F3 cells Concentration: 1 nM, 10nM, 100 nM, 1 μM and 10 μM Incubation Time: 72 hours Result: The GI50s for Ba/F3 FLT3-ITD cells and parental Ba/F3 cells are 0.034±0.015 μM and 1.136±0.389 μM, respectively. Western Blot Analysis Cell Line: MV4-11 cells Concentration: 0.01, 0.1, 1, 10 and 100 nM Incubation Ti

体内研究：

A single dose of FLT3-IN-3 (Compound 7d; 10 mg/kg; i.p.) in mice with subcutaneous MV4-11 xenografts causes sustained inhibition of FLT3 and STAT5 phosphorylation over 48 hours. Animal Model: Female athymic nu/nu mice with subcutaneously implanted MV4-11 xenografts Dosage: 10 mg/kg Administration: Intraperitoneal (i.p.) injection; 48 hours Result: Effectively inhibited FLT3-ITD autophosphorylation in MV4-11 xenografts.

参考文献：

1. Gucký T, et al. Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations. J Med Chem. 2018 May 10;61(9):3855-3869.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.039 ml	10.197 ml	20.395 ml
5 mM	0.408 ml	2.039 ml	4.079 ml
10 mM	0.204 ml	1.02 ml	2.039 ml
50 mM	0.041 ml	0.204 ml	0.408 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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