SD-36|cas:2429877-44-9|西域试剂

SD-36,99.46%

产品编号：Bellancom-129602| CAS NO：2429877-44-9| 分子式：C₅₉H₆₂F₂N₉O₁₂P| 分子量：1158.15

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-129602	￥27000.00	杭州北京（现货）
Bellancom-129602	￥38000.00	杭州北京（现货）
Bellancom-129602	￥62000.00	杭州北京（现货）

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SD-36

产品介绍

SD-36 是一种有效的 STAT3 PROTAC 降解剂 (K_d=~50 nM)，与其他 STAT 成员相比具有很高的选择性。SD-36 有效降解细胞中突变的 STAT3 蛋白，并抑制 STAT3 的转录活性 (IC₅₀=10 nM)。SD-36 发挥强大的抗肿瘤活性，并在小鼠肿瘤模型中实现了完整而持久的肿瘤消退。SD-36 由 STAT3 抑制剂 SI-109、 linker 和一个用于 E3 泛素连接酶的 Cereblon 配体 Lenalidomide 类似物组成。

生物活性

SD-36 is a potent and efficacious STAT3 PROTAC degrader (K_d=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC₅₀=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase.

体外研究

SD-36 inhibits the growth of a subset of acute myeloid leukemia and anaplastic large-cell lymphoma cell lines by inducing cell-cycle arrest and/or apoptosis.
SD-36 (0.005-5 μM; 4 days) demonstrates potent activity (IC₅₀＜2 μM) in MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines.
SD-36 (1 μM; 5 hours) completely depletes both monomeric and dimeric STAT3 protein in MOLM-16 cells.

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

Cell Viability Assay

Cell Line:	MOLM-16, DEL, Karpas-299, KI-JK, SU-DHL-I, SUP-M2 cell lines
Concentration:	0.005, 0.05, 0.5, 5 μM
Incubation Time:	4 days
Result:	Demonstrated potent activity (IC₅₀＜2 μM) in those cell lines.

Western Blot Analysis

Cell Line:	MOLM-16 cells
Concentration:	1 μM
Incubation Time:	5 hours
Result:	Completely depletes both monomeric and dimeric STAT3 protein.

体内研究
(In Vivo)

SD-36 (25-100 mg/kg; i.v.; weekly dosing for 4 weeks) achieves complete and long-lasting tumor regression in mice.
SD-36 effectively inhibits tumor growth at 25 and 50 mg/kg administered on day 1, 3, and 5 per week and achieved complete tumor regression at 100 mg/kg with the same schedule in the SU-DHL-1 xenograft model.
SD-36 at 50 mg/kg 3 times per week completely inhibits tumor growth in the SUP-M2 tumor model.

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

Animal Model:	SCID female mice (MOLM-16 xenograft model)
Dosage:	25, 50, 100 mg/kg
Administration:	i.v.; weekly dosing for 4 weeks
Result:	At 25 and 50 mg/kg weekly dosing for 4 weeks effectively inhibited tumor growth. At either 100 mg/kg weekly or 50 mg/kg twice weekly for 4 weeks induced complete tumor regression.

体内研究

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

Animal Model:	SCID female mice (MOLM-16 xenograft model)
Dosage:	25, 50, 100 mg/kg
Administration:	i.v.; weekly dosing for 4 weeks
Result:	At 25 and 50 mg/kg weekly dosing for 4 weeks effectively inhibited tumor growth. At either 100 mg/kg weekly or 50 mg/kg twice weekly for 4 weeks induced complete tumor regression.

体内研究

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

Animal Model:	SCID female mice (MOLM-16 xenograft model)
Dosage:	25, 50, 100 mg/kg
Administration:	i.v.; weekly dosing for 4 weeks
Result:	At 25 and 50 mg/kg weekly dosing for 4 weeks effectively inhibited tumor growth. At either 100 mg/kg weekly or 50 mg/kg twice weekly for 4 weeks induced complete tumor regression.

性状

Solid

溶解性数据

In Vitro:

DMSO : 150 mg/mL (129.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.8634 mL	4.3172 mL	8.6345 mL
5 mM	0.1727 mL	0.8634 mL	1.7269 mL
10 mM	0.0863 mL	0.4317 mL	0.8634 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 (stored under nitrogen)。-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: ≥ 5 mg/mL (4.32 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (4.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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。
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% corn oil
Solubility: ≥ 5 mg/mL (4.32 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (4.32 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。