FLT3-IN-3|cas:2229050-90-0|西域试剂

FLT3-IN-3,99.73%

产品编号：Bellancom-112145| CAS NO：2229050-90-0| 分子式：C₂₇H₃₈N₈O| 分子量：490.64

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货号	价格	库存与货期
Bellancom-112145	￥2600.00	杭州北京（现货）
Bellancom-112145	￥4400.00	杭州北京（现货）
Bellancom-112145	￥7900.00	杭州北京（现货）
Bellancom-112145	￥11000.00	杭州北京（现货）

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FLT3-IN-3

产品介绍

FLT3-IN-3 是一种有效的 FLT3 抑制剂，抑制 FLT3 WT 和 FLT3 D835Y，IC₅₀ 分别为 13 和 8 nM。

生物活性

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

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.

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

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 Time:	1 hours
Result:	Concentrations as low as 1 nM were sufficient to block the autophosphorylation of the FLT3 receptor tyrosine kinase at three different tyrosine residues (589, 591, and 842).

体内研究
(In Vivo)

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.

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

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.

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.

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

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.

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.

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

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (509.54 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0382 mL	10.1908 mL	20.3815 mL
5 mM	0.4076 mL	2.0382 mL	4.0763 mL
10 mM	0.2038 mL	1.0191 mL	2.0382 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.24 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.24 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.24 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。