2502156-03-6
基本信息
PROTAC KRASG12C Degrader-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-m
(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
物理化學(xué)性質(zhì)
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/11/08 | 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?；?哌嗪-1-基)-5,6,7,8-四氫吡啶并[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-羥基-N-(4-(4-甲基噻唑-5-基)芐基)吡咯烷-2-甲酰胺 LC-2 | 2502156-03-6 | 1mg | 3000元 |
| 2024/08/19 | 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?；?哌嗪-1-基)-5,6,7,8-四氫吡啶并[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?；?-4-羥基-N-(4-(4-甲基噻唑-5-基)芐基)吡咯烷-2-甲酰胺 LC-2 | 2502156-03-6 | 5mg | 9800元 |
| 2022/09/18 | 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?；?哌嗪-1-基)-5,6,7,8-四氫吡啶并[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-羥基-N-(4-(4-甲基噻唑-5-基)芐基)吡咯烷-2-甲酰胺 LC-2 | 2502156-03-6 | 10mg | 25000元 |
常見問(wèn)題列表
|
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 |