PROTAC KRASG12C Degrader-LC-2
| 中文名稱 | PROTAC KRASG12C Degrader-LC-2 |
|---|---|
| 中文同義詞 | (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|||PROTAC KRASG12C DEGRADER-LC-2|||LC2;化合物L(fēng)C-2;LC-2 ,S6996 |
| 英文名稱 | PROTAC KRASG12C Degrader-LC-2 |
| 英文同義詞 | 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-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;L-Prolinamide, N-[3-[3-[(2S)-2-[[[7-(8-chloro-1-naphthalenyl)-4-[(3S)-3-(cyanomethyl)-4-(2-fluoro-1-oxo-2-propen-1-yl)-1-piperazinyl]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl]oxy]methyl]-1-pyrrolidinyl]propoxy]-1-oxopropyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-;LC-2 ，S6996;LC-2 |
| CAS號 | 2502156-03-6 |
| 分子式 | C59H71ClFN11O7S |
| 分子量 | 1132.78 |
| EINECS號 | |
| 相關(guān)類別 | |
| Mol文件 | 2502156-03-6.mol |
| 結(jié)構(gòu)式 |  |
PROTAC KRASG12C Degrader-LC-2 性質(zhì)
| 密度 | 1.297±0.06 g/cm3(Predicted) |
|---|---|
| 儲存條件 | Store at -20°C |
| 溶解度 | DMSO：50 mg/mL（44.14 mM；超聲加熱并加熱至 80°C） |
| 形態(tài) | 固體 |
| 酸度系數(shù)(pKa) | 14.07±0.40(Predicted) |
| 顏色 | 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 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2026/06/05 | 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 | 1mg | 3000元 |
| 2026/06/05 | HY-137516 | PROTAC KRASG12C Degrader-LC-2 LC-2 | 2502156-03-6 | 10 mM * 1 mL in DMSO | 18691元 |