SF2523 - CAS:1174428-47-7

您当前的位置：

SF2523

目录号 : KM5818 CAS No. : 1174428-47-7 纯度 : 97%

Data Sheet 产品使用指南

SF2523 是一种有效的选择性 PI3K 抑制剂，抑制 PI3Kα，PI3Kγ，DNA-PK，BRD4 和 mTOR，IC₅₀ 分别为 34 nM，158 nM，9 nM，241 nM 和 280 nM。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

查看所有商品（2）

加入购物车大包装询价

Other Forms of Rapamycin:

Ginkgolide B In-stock
Isoginkgetin In-stock
Ginkgolic acid C17:1 In-stock
Ginkgolic Acid In-stock
Propargyl-PEG4-amine In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

SF2523 is a highly selective and potent inhibitor of PI3K with IC₅₀s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

体外研究

SF2523 treatment decreases protein levels of MYCN and Cyclin D1, the MYCN target, and inhibits AKT activation by blocking phosphorylation of AKT at Ser473. SF2523 treatment leads to the displacement of BRD4 from both MYCN promoter sites. SF2523 interacts robustly with the full-length BRD4 (K_d=140 nM) and exhibits comparable affinity to the BRD4 first BD (BD1) (K_d=150 nM), however it binds more weakly to the second BD (BD2) of BRD4 (K_d=710 nM). Comparison of binding affinities of SF2523 for BDs of other proteins reveal that it binds equally well to BDs of BRD4, BRD2, and BRD3; shows moderate binding to BDs of CECR2 and BRDT; but associates much weaker with other BDs.

体内研究

SF2523 treatment results in a significant reduction of tumor volume compared with control. Importantly, SF2523 shows no gross toxicity to the treated mice, as there is no notable change in body weight. Tumors from SF2523-treated mice have markedly reduced MYCN, pAKT, and Cyclin D1 levels compared with levels of these proteins in vehicle-treated mice tumors.

分子式

C₁₉H₁₇NO₅S

分子量

371.41

CAS号

1174428-47-7

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 : ≥ 30 mg/mL (80.77 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6924 mL	13.4622 mL	26.9244 mL
5 mM	0.5385 mL	2.6924 mL	5.3849 mL
10 mM	0.2692 mL	1.3462 mL	2.6924 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 (6.73 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.73 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 (6.73 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.73 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。