PROTAC KRASG12C Degrader-LC-2
- CAS号:2502156-03-6
- 英文名:PROTAC KRASG12C Degrader-LC-2
- 中文名:PROTAC KRASG12C Degrader-LC-2
- CBNumber:CB78200421
- 分子式:C59H71ClFN11O7S
- 分子量:1132.78
- MOL File:Mol file
- 密度 :1.297±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: 50 mg/mL (44.14 mM; ultrasonic and warming and heat to 80°C)
- 形态 :Solid
- 酸度系数(pKa) :14.07±0.40(Predicted)
- 颜色 :Off-white to brown
PROTAC KRASG12C Degrader-LC-2性质、用途与生产工艺
- 生物活性 LC-2 是首创的内源性 KRAS G12C 的 PROTAC 降解剂,DC50 在 0.25 和 0.76 μM 之间。LC-2 是一种 PROTAC,与 MRTX849 共价结合 KRAS G12C 并招募 E3 连接酶 VHL,诱导 KRAS G12C 快速持续降解,导致纯合和杂合子 KRAS G12C 细胞系 MAPK 信号的抑制。
-
靶点
KRAS(G12C)
0.25-0.76 μM (DC 50 )
VHL
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体外研究
LC-2 induces degradation of endogenous KRASG12C in multiple KRAS mutant cancer cell (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23 and NCI-H358 cells) with DC 50 s between 0.25 and 0.76 μM. LC-2-induced KRASG12C degradation occurs via a bona fide PROTAC mechanism. MIA PaCa-2, NCI-H23, and SW1573 cells are treated with 2.5 μM of LC-2 for 6, 24, 48, and 72 h. In all three cell lines, maximal KRAS degradation occurred within 24 h and was sustained up to 72 h.
LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modulates Erk signaling in homozygous and heterozygous KRAS mutant cell lines.Western Blot Analysis
Cell Line: MIA PaCa-2 cells and NCI-H23 cells Concentration: 2.5 μM Incubation Time: 6-24 hours Result: Inhibition and degradation of KRAS G12C decreases pErk signaling at 6 and 24 h in homozygous MIA PaCa-2 cells
- 更新日期:2024/11/08
- 产品编号:HY-137516
- 产品名称:(2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-氯萘-1-基)-4-((S)-3-(氰基甲基)-4-(2-氟丙烯酰基)哌嗪-1-基)-5,6,7,8-四氢吡啶并[3,4-D]嘧啶-2-基)氧基)甲基)吡咯烷-1- 基)丙氧基)丙酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺 LC-2
- CAS编号:2502156-03-6
- 包装:1mg
- 价格:3000元
- 更新日期:2024/08/19
- 产品编号:HY-137516
- 产品名称:(2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-氯萘-1-基)-4-((S)-3-(氰基甲基)-4-(2-氟丙烯酰基)哌嗪-1-基)-5,6,7,8-四氢吡啶并[3,4-D]嘧啶-2-基)氧基)甲基)吡咯烷-1- 基)丙氧基)丙酰胺基)-3,3-二甲基丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺 LC-2
- CAS编号:2502156-03-6
- 包装:5mg
- 价格:9800元
- 公司名称:Aladdin Scientific
- 联系电话:+1-+1(833)-552-7181
- 电子邮件:sales@aladdinsci.com
- 国家:美国
- 产品数:52924
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58