SD-436

CAS: 2497585-50-7 F: C58H62F4N9O14PS W: 1248.20

SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (

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Bioactivity	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].
Invitro	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. 0 --> SD-436 相关抗体: Western Blot Analysis[1] Cell Line:
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Species
CAS	2497585-50-7
Formula	C58H62F4N9O14PS
Molar Mass	1248.20
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Xu, et al. Discovery of SD-436: A Potent, Highly Selective and Efficacious STAT3 PROTAC Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression. Journal of medicinal chemistry. 2024, 67(22), 20495–20513.