2. PROTAC Stem Cell/Wnt JAK/STAT Signaling
  3. PROTACs STAT
  4. SD-436

SD-436 是一种高选择性和高效的 STAT3 PROTAC 降解剂 (DC50为 0.5 μM)，对 STAT3、STAT1、STAT4、STAT5 和 STAT6 的 IC50 分别为 19 nM、270 nM、360 nM、>10 μM 和 >10 μM。SD-436 可促进 STAT3 的泛素化和降解，且诱导肿瘤消减。SD-436 可用于肿瘤研究，例如白血病和淋巴瘤 (粉红：STAT3 配体 (HY-169361)；蓝色：E3 连接酶配体 (HY-43722)；黑色：连接子 (HY-147052)。

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SD-436 Chemical Structure

SD-436 Chemical Structure

CAS No. : 2497585-50-7

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SD-436 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 STAT 亚型特异性产品:

查看所有亚型
STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma (Pink: STAT3 ligand (HY-169361); Blue: E3 ligase ligand (HY-43722); Black: linker (HY-147052)[1].

IC50 & Target[1]

Cereblon

 

STAT3

19 nM (IC50)

STAT1

270 nM (IC50)

STAT5

>10 μM (IC50)

STAT6

>10 μM (IC50)

体外研究
(In Vitro)

SD-436 抑制 MOLM-16 白血病细胞系、SU-DHL-1 和 SUP-M2 淋巴瘤细胞系的生长， IC50分别为 0.038 μM、0.43 μM 和 0.39 μM[1]。
SD-436 (0.1 nM-40 μM, 20 h) 可降低人 PBMC、SU-DHL-1 和 MOLM-16 细胞系中 STAT3 蛋白的水平[1]。
SD-436 (0.1 nM-40 μM, 20 h) 以剂量依赖的方式有效降低 Pfeiffer 细胞系中突变 STAT3 (STAT3K658R) 蛋白的水平，DC50 值为 2.5 nM[1]。
SD-436 在小鼠、大鼠、狗、猴子和人类血浆中表现出极好的稳定性，T1/2 大于 120 min[1]。
SD-436 对人类 ether-a-go-go 相关基因钾通道无明显抑制作用 (hERG 抑制率：3 μM 时为 1.3%，30 μM 时为 1.1%)[1]。

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

SD-436 相关抗体:

Western Blot Analysis[1]

Cell Line: PBMC, MOLM-16, SU-DHL-1 and Pfeiffer
Concentration: 0.1 nM, 0.5 nM, 2.5 nM, 13 nM, 64 nM, 320 nM, 1600 nM, 8000 nM, 40000 nM
Incubation Time: 20 h
Result: Reduced the levels of STAT3 protein in human PBMCs and SU-DHL-1 cell line, with DC50 of 0.1 nM and 10 nM, respectively.
Achieved near complete degradation at 320 nM with merely a 4 h treatment time in the MOLM-16 cell line.
Reduced the levels of the mutated STAT3 protein in a dose-dependent manner in the Pfeiffer cell line, with a DC50 value of 2.5 nM.
Showed high selectivity for STAT3 over other STAT proteins.
体内研究
(In Vivo)

SD-436 (5 mg/kg，静脉注射，单次) 可有效诱导小鼠正常组织（肝脏和脾脏）和 MOLM-16 异种移植肿瘤组织中 STAT3 的快速、完全和持久消减[1]。
SD-436 (5-25 mg/kg，静脉注射) 在白血病和淋巴瘤异种移植小鼠模型中显示出抗肿瘤活性[1]。
SD-436 在小鼠、大鼠和狗体内的药代动力学

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

Species IV dose (mg/kg) t1/2 (h) Cmax (ng/mL) AUC(0-t) (h × ng/mL) Vz (L/kg) CI (mL/min/kg) Cl (%HBF)
ICR mouse 5 22.1 130,185 859,223 0.10 0.051 0.1%
SD rat 5 1.0 82,626 59,484 0.12 1.4 2.6%
beagle dog 1 2.3 8861 10,699 0.29 1.5 2.7%
Animal Model: MOLM-16 acute leukemia xenograft model and the SU-DHL-1 lymphoma xenograft model in SCID mice (injected subcutaneously with 3 × 106 MOLM-16 cells or 5 × 106 SU-DHL-1 cells)[1]
Dosage: 5, 10, 20 mg/kg (MOLM-16); 10, 25 mg/kg (SU-DHL-1)
Administration: Intravenous injection (i.v.); once a week, four weeks (MOLM-16: 5, 10, 20 mg/kg; SU-DHL-1: 10, 25 mg/kg) or twice a week, four weeks (SU-DHL-1: 25 mg/kg)
Result: Showed that SD-436 at 5 mg/kg was able to achieve a maximum of 76% tumor regression in the MOLM-16 leukemia xenograft model.
Induced complete tumor regression at 10 and 20 mg/kg in the MOLM-16 leukemia xenograft model.
Achieved complete and long-lasting tumor regression in the SU-DHL-1 xenograft model at 25 mg/kg weekly dosing schedule.
分子量

1248.20

Formula

C58H62F4N9O14PS
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

SD-436 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

SD-4362497585-50-7SD436SD 436PROTACsSTATLeukemiaLymphomaMOLM-16ICRPermeabilityXenograftInhibitorinhibitorinhibit

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