SD-36 ( —— )

产品货号. M33557 CAS No. 2429877-44-9

SD-36 是一种有效的 STAT3 PROTAC 降解剂 (Kd=~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。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
500MG	获取报价	有现货
1G	获取报价	有现货

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生物学信息

产品名称

SD-36
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

SD-36 是一种有效的 STAT3 PROTAC 降解剂 (Kd=~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。
产品描述

SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~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. SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体外实验

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.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.
体内实验

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. 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.
同义词

——
通路

Apoptosis
靶点

Apoptosis
受体

Apoptosis | STAT
研究领域

——
适应症

——

化学信息

CAS Number

2429877-44-9
分子量

1158.15
分子式

C59H62F2N9O12P
纯度

>98% (HPLC)
溶解度

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (43.17 mM; 超声助溶 )
SMILES

C(N[C@H](C(NC(C1=CC=CC=C1)C2=CC=CC=C2)=O)CCC(N)=O)(=O)[C@H]3N4[C@](CC3)(CCN(C(CCCCCC#CC5=C6C(C(=O)N(C6)C7C(=O)NC(=O)CC7)=CC=C5)=O)C[C@H](NC(=O)C8=CC=9C(N8)=CC=C(C(P(=O)(O)O)(F)F)C9)C4=O)[H]
化学全称

——

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

参考文献

1. Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36(5):498-511.e17.?

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