SKLB4771 FLT3-IN-1|cas:1370256-78-2|西域试剂

SKLB4771 FLT3-IN-1,98.08%

产品编号：西域-12960| CAS NO：1370256-78-2| 分子式：C₂₅H₂₇N₇O₃S₂| 分子量：537.66

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货号	价格	库存与货期
西域-12960	￥2333.00	杭州北京（现货）
西域-12960	￥3500.00	杭州北京（现货）
西域-12960	￥5000.00	杭州北京（现货）

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SKLB4771 FLT3-IN-1

生物活性

SKLB4771 is a potent and selective Flt3 inhibitor with an IC₅₀ value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue.

IC₅₀ & Target

IC50: 10 nM (Flt3); 3.7 μM (Flt4); 1.5 μM (Aurora A); 6.8 μM (c-kit); 2.8 μM (FMS)

体外研究
(In Vitro)

SKLB4771 (compound 20c) (72 h) inhibits FLT3-ITD-expressing MV4-11 cells with an IC₅₀ value of 6 nM, and inhibits other cancer cells with IC₅₀s of 3.05 μM (Jurkat), 6.25 μM (Ramos), 3.72 μM (PC-9), 6.94 μM (H292), and 8.91 μM (A431), respectively.
SKLB4771 (0-300 nM; 20 h) inhibits FLT3 phosphorylation and also decreases the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 at concentrations >0.1 μM.

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

Western Blot Analysis

Cell Line:	MV4-11 cells
Concentration:	0, 30, 100, 300 nM
Incubation Time:	20 hours
Result:	Resulted inhibition against the human FLT3 kinase in a dose-dependent manner, and decreased the phosphorylation level of STAT5 and ERK1/2 at 100 nM and 300 nM.

体内研究
(In Vivo)

SKLB4771 (20-100 mg/kg; i.p.; once daily; 21 d) inhibits tumor growth in vivo without significant weight loss or any other obvious signs of toxicity on mice.
Pharmacokinetic Analysis of SKLB4771 in rat (40 mg/kg; i.p.)

C_max (μg/mL)	T_1/2 (h)	AUC_max (h·μg/mL)	T_max (h)	CL_obs (L/h/kg)
5.31	13.9	21.86	1.0	2.21

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

Animal Model:	Female NOD-SCID mouse (6−7 weeks old)
Dosage:	20, 40, 100 mg/kg; dissolved in 25% (v/v) PEG400 plus 5% DMSO, administered at a dose of 5 mL/kg
Administration:	Intraperitoneal injection; once daily; 21 days
Result:	Inhibited tumor growth by 66% and 84% at concentration of 20 mg/kg and 40 mg/kg, respectively. Resulted cell proliferation inhibition and apoptosis induction.

分子量

537.66

性状

Solid

Formula

C₂₅H₂₇N₇O₃S₂

CAS 号

1370256-78-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (61.99 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8599 mL	9.2996 mL	18.5991 mL
5 mM	0.3720 mL	1.8599 mL	3.7198 mL
10 mM	0.1860 mL	0.9300 mL	1.8599 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: ≥ 2.5 mg/mL (4.65 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.65 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
2.
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (4.65 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (4.65 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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。
3.
请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.65 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度 & 产品资料

纯度： 98.08%

参考文献

. Li WW, et al. Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. J Med Chem. 2012 Apr 26;55(8):3852-66. [Content Brief]
. Yan HX, et al. Accumulation of FLT3(+) CD11c (+) dendritic cells in psoriatic lesions and the anti-psoriatic effect of a selective FLT3 inhibitor. Immunol Res. 2014 Oct;60(1):112-26. [Content Brief]

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SKLB4771 FLT3-​IN-​1,98.08%

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SKLB4771 FLT3-IN-1,98.08%

SKLB4771 FLT3-IN-1