1. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  2. PROTACs STAT
  3. SD-2301

SD-2301 是一种选择性的 STAT3 PROTAC 降解剂。SD-2301 诱导 STAT3 降解,而不影响其他 STAT 家族成员(STAT1、STAT2、STAT4、STAT5、STAT6)的蛋白水平。SD-2301 在携带 B16F10 的小鼠中发挥抗肿瘤作用。SD-2301 可用于癌症研究。(粉红色:STAT3 配体 (HY-172947),蓝色:VHL 配体 (HY-172948),黑色:连接子 (HY-W577012),VHL 配体-连接子偶联物 (HY-172949))。

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SD-2301

SD-2301 Chemical Structure

CAS No. : 3054116-24-1

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  • 生物活性

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  • 参考文献

生物活性

SD-2301 is a selective STAT3 PROTAC degrader. SD-2301 induces STAT3 degradation without affecting the protein levels of other STAT family members (STAT1, STAT2, STAT4, STAT5, STAT6). SD-2301 exerts anti-tumor effects in B16F10-bearing mice. SD-2301 can be used for the study of cancer. (Pink: STAT3 ligand (HY-172947), Blue: VHL Ligand (HY-172948), Black: Linker (HY-W577012), VHL ligand-linker conjugate (HY-172949))[1].

IC50 & Target[1]

STAT3

 

VHL

 

体外研究
(In Vitro)

SD-2301 (50 nM, 24 h) 有效降解小鼠树突状细胞 (DCs) 中的 STAT3 蛋白[1]
SD-2301 (0.32-200 nM, 14 h) 在人外周血单核细胞 (PBMCs) 中表现出高潜能和选择性,诱导 STAT3 降解,而不影响其他 STAT 蛋白 (STAT1, STAT2, STAT4, STAT5, STAT6)[1]

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

体内研究
(In Vivo)

SD-2301 (5 mg/kg,静脉注射,每 3 天一次,4 周) 在小鼠中显示出抑制 B16F10 黑色素瘤生长的效能[1]
SD-2301 (5 mg/kg,静脉注射,每 3 天一次) 增加 MC38 荷瘤 C57BL/6J 小鼠肿瘤浸润淋巴细胞中 KSPWFTTL tetramer+CD8+ T 细胞的比例[1]

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

Animal Model: B16F10 cells (2 × 105) were subcutaneously implanted into the flanks of 6-8-week-old C57BL/6J mice[1]
Dosage: 5 mg/kg
Administration: i.v., once every 3 days, 4 weeks
Result: Exhibited potency in inhibiting tumor growth.
Increased the number of effector CD8+ T cells (IFNγ+, GZMB+) in tumors.
Showed no significant changes in body weight.
Degraded STAT3 protein.
分子量

1366.50

Formula

C64H80N13O15PS2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SD-2301
目录号:
HY-172946
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