规格

价格

库存

数量

1 mg

¥ 1,900

现货

5 mg

¥ 4,180

现货

10 mg

¥ 6,270

现货

50 mg

¥ 13,800

现货

生物活性

产品描述	Setidegrasib is a PROTAC-mediated KRAS degrader (DC50: 37 nM). Setidegrasib induces the formation of a ternary complex between KRAS G12D and the VHL E3 ubiquitin ligase, thereby facilitating the ubiquitination and proteasomal degradation of the oncogenic protein. Setidegrasib inhibits the levels of p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates antitumor activity in various mouse xenograft models of cancer. Setidegrasib can be used to study solid tumors with KRAS(G12D) mutations.
体外活性	方法：多种KRAS(G12D)突变癌细胞（AsPC-1, PK-59, HPAC, GP2d, GP5d等）与 KRAS WT 细胞（A375、HT-29、BxPC-3、COLO-320）加入Setidegrasib (0.1 nM – 10 μM)处理6天，CellTiter-Glo 2.0实验检测ATP。结果：Setidegrasib 强效抑制多种 KRAS(G12D) 突变癌细胞系的增殖，而对 KRAS(WT) 细胞 (A375, HT-29) 及其他 KRAS 突变体 (G12V, G12C, G13D) 的活性较弱 (IC50 > 10 μM)。[1]
体内活性	方法：为研究Setidegrasib 抗肿瘤活性，构建LXFA 1125肺癌PDX模型（裸鼠），静脉注射Setidegrasib (10、30 mg/kg )，每周2次，持续21天。结果：Setidegrasib 剂量依赖性抑制肿瘤生长；IHC显示KRAS(G12D)表达降低。[1]
别名	KRAS G12D inhibitor 17, ASP-3082, ASP3082, ASP 3082

化学信息

分子量	1117.30
分子式	C₆₀H₆₅FN₁₂O₇S
CAS No.	2821793-99-9
Smiles	O(CC1=CC=C(C=C1)C2=CN([C@H](C(=O)N3[C@H](C(N[C@@H](CO)C4=CC=C(C=C4)C5=C(C)N=CS5)=O)C[C@@H](O)C3)[C@H](C)C)N=N2)C6=C(C(=CC7=C6N=C(OC8CCOCC8)N=C7N9[C@]%10(C[C@@](C9)(NC%10)[H])[H])C%11CC%11)C%12=C%13C(=CC(F)=C%12C)NN=C%13

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 80.00 mg/mL (71.60 mM), Sonication is recommended.

溶液配制表

DMSO

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Setidegrasib