PROTAC KRASG12C Degrader-LC-2
| 中文名称 | PROTAC KRASG12C Degrader-LC-2 |
|---|---|
| 中文同义词 | (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|||PROTAC KRASG12C DEGRADER-LC-2|||LC2 |
| 英文名称 | PROTAC KRASG12C Degrader-LC-2 |
| 英文同义词 | PROTAC KRASG12C Degrader-LC-2;LC-2;(2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-Chloronaphthalen-1-yl)-4-((S)-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;(2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-Chloronaphthalen-1-yl)-4-((S)-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-m |
| CAS号 | 2502156-03-6 |
| 分子式 | C59H71ClFN11O7S |
| 分子量 | 1132.78 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | Mol File |
| 结构式 |
PROTAC KRASG12C Degrader-LC-2 性质
| 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；超声加热并加热至 80°C） |
| 形态 | 固体 |
| 酸度系数(pKa) | 14.07±0.40(Predicted) |
| 颜色 | 米白色至棕色 |
|
KRAS(G12C) 0.25-0.76 μM (DC 50 ) |
VHL
|
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 |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-137516 | (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 | 2502156-03-6 | 1mg | 3200元 |
| 2024/04/30 | HY-137516 | (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 | 2502156-03-6 | 5mg | 9800元 |