【K-Ras 特異性降解劑、抑制劑和拮抗劑】K-Ras Specific Degraders, Inhibitors & Antagonists-MCE
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K-Ras 特異性降解劑、抑制劑和拮抗劑-K-Ras Specific Degraders, Inhibitors & Antagonists
Kirsten 大鼠肉瘤病毒癌基因同系物 (KRAS) 是 RAS-MAPK 通路的原癌基因，有 30% 的癌症與 RAS 基因突變過度活化相關，其中有高達 85% 的比例是由 RAS 蛋白異構體 (Isoform)「KRAS」突變所引起。KRAS 突變存在於多種實體腫瘤中，包括肺腺癌、結直腸癌和導管胰腺癌。在 KRAS 突變引起的腫瘤中，有 80% 的突變是發生在 KRAS 蛋白序列的第 12 個胺基酸上：G12D (41%)、G12V (28%)、G12C (14%)。RAS致癌基因是人類癌症中突變最頻繁的致癌基因，也是 1982 年發現的第一個確認的人類致癌基因。經過數十年的研究，Shokat 實驗室在 2013 年取得了重大突破，表明由KRAS基因中的 G12C 突變可以通過新發現的開關 II 口袋直接抑制。基於這一突破性發現，sotorasib (AMG510) 於 2021 年獲得美國食品和藥物管理局的批准，成為第一個直接靶向 KRAS 癌蛋白治療任何 KRAS 突變癌症的療法，尤其是那些攜帶 KRAS G12C 突變的癌症。自 1960 年代發現 KRAS 以來，最近在治療 KRAS 驅動的癌症患者方面進展甚微。在一段時間內，人們認為直接靶向 KRAS 的可能性不大，因此認為 KRAS 是“不可抗藥的”，Shokat 實驗室在 2013 年發現了 KRAS G12C switch II pocket ，從而重振了對直接 KRAS 抑制劑的研究。
MCE (MedChem Express)
MCE總部位於美國新澤西，提供種類齊全的化學及生化研究用產品，包括創新的生命科學試劑，reference compounds(標準化合物)，APIs(原料藥)及Natural compounds(天然化合物)以提供實驗室或科學研究之用，MedChemExpress(MCE)產品50000+ 特異性抑制劑、化合物庫、重組蛋白，專注於信號通路和疾病研究領域。全球文獻廣泛引用，質控體系嚴格，品質100%。
K-Ras Specific Degraders, Inhibitors & Antagonists
| Product Name | K-Ras Selectivity | Purity |
|---|---|---|
| Sotorasib | Selective Inhibitor | 99.94% |
| Adagrasib | Selective Inhibitor | 99.93% |
| MRTX1133 | Selective Inhibitor | 99.42% |
| BI-2852 | Selective Inhibitor | 98.74% |
| BI-3406 | Selective Inhibitor | 99.95% |
| BAY-293 | Selective Inhibitor | 98.06% |
| LC-2 | Selective Inhibitor | |
| ARS-1620 | Selective Inhibitor | 98.80% |
| Opnurasib | Selective Inhibitor | 98.94% |
| MRTX-1257 | Selective Inhibitor | 99.14% |
| MRTX0902 | Selective Inhibitor | 99.45% |
| Divarasib | Selective Inhibitor | 99.46% |
| PROTAC K-Ras Degrader-1 | Selective Inhibitor | 98.05% |
| Sotorasib racemate | Selective Inhibitor | 98.99% |
| ARS-853 | Selective Inhibitor | 98.39% |
| ASP2453 | Selective Inhibitor | 98.04% |
| ARS-1323-alkyne | Selective Inhibitor | 99.59% |
| ARS-1630 | Selective Inhibitor | 98.10% |
| AZD4625 | Selective Inhibitor | 99.52% |
| ARS-1323 | Selective Inhibitor | 99.14% |
| KRAS G12D inhibitor 14 | Selective Inhibitor | 99.39% |
| G12Si-5 formic | Selective Inhibitor | |
| K-Ras G12C-IN-2 | Selective Inhibitor | 99.21% |
| KRAS inhibitor-6 | Selective Inhibitor | |
| KRAS inhibitor-8 | Selective Inhibitor | |
| KRAS inhibitor-7 | Selective Inhibitor | |
| KRAS G12C inhibitor 28 | Selective Inhibitor | 99.94% |
| KRAS G12C inhibitor 27 | Selective Inhibitor | |
| KRAS G12C inhibitor 15 | Selective Inhibitor | 99.55% |
| KRAS G12C inhibitor 32 | Selective Inhibitor | |
| G12Si-1 | Selective Inhibitor | |
| SOS1-IN-15 | Selective Inhibitor | |
| KRAS G12C inhibitor 5 | Selective Inhibitor | |
| KRAS G12C inhibitor 18 | Selective Inhibitor | |
| KRAS G12C inhibitor 13 | Selective Inhibitor | |
| KRAS inhibitor-20 | Selective Inhibitor | |
| KRAS G12C inhibitor 17 | Selective Inhibitor | |
| KRAS G12D inhibitor 3 | Selective Inhibitor | |
| KRAS G12C inhibitor 16 | Selective Inhibitor | |
| KRAS G12C inhibitor 14 | Selective Inhibitor | 98.07% |
| Spiclomazine hydrochloride | Selective Inhibitor | |
| BI-0474 | Selective Inhibitor | |
| KRas G12C inhibitor 4 | Selective Inhibitor | |
| KRas G12C inhibitor 1 | Selective Inhibitor | |
| SOS1-IN-10 | Selective Inhibitor | |
| KRAS G12C inhibitor 23 | Selective Inhibitor | |
| KRAS G12C inhibitor 25 | Selective Inhibitor | |
| MRTX849 acid | Selective Inhibitor | |
| KRAS G12C inhibitor 57 | Selective Inhibitor | |
| G12Si-5 | Selective Inhibitor | |
| SOS1-IN-4 | Selective Inhibitor | |
| KRAS G12C inhibitor 50 | Selective Inhibitor | |
| MRTX849 ethoxypropanoic acid | Selective Antagonist | |
| KRas G12C inhibitor 3 | Selective Inhibitor | |
| K20 | Selective Inhibitor | |
| KRAS G12D inhibitor 7 | Selective Inhibitor | |
| KRAS G12D inhibitor 16 | Selective Inhibitor | |
| SOS1-IN-9 | Selective Inhibitor | |
| KRas G12C inhibitor 2 | Selective Inhibitor | |
| PROTAC SOS1 degrader-3 | Selective Inhibitor | |
| KRAS G12D inhibitor 3 TFA | Selective Inhibitor | |
| KRAS inhibitor-11 | Selective Inhibitor | |
| KRAS G12C inhibitor 26 | Selective Inhibitor | |
| KRAS G12C inhibitor 24 | Selective Inhibitor | |
| 6H05 | Selective Inhibitor | |
| MRTX-EX185 formic | Pan Inhibitor | |
| Pan KRas-IN-1 | Pan Inhibitor | 98.47% |
| SAH-SOS1A TFA | Pan Inhibitor | 99.16% |
| KRpep-2d | Pan Inhibitor | |
| KRAS inhibitor-10 | Pan Inhibitor | 99.86% |
| KRpep-2d TFA | Pan Inhibitor | 98.11% |
| KRAS inhibitor-16 | Pan Inhibitor | |
| SOS1-IN-8 | Pan Inhibitor | |
| KRAS inhibitor-14 | Pan Inhibitor | |
| KRAS G12C inhibitor 49 | Pan Inhibitor | |
| KRAS inhibitor-13 | Pan Inhibitor | |
| KRAS G12C inhibitor 52 | Pan Inhibitor | |
| KRAS inhibitor-12 | Pan Inhibitor | |
| SOS1-IN-7 | Pan Inhibitor | |
| RAS-IN-2 | Pan Inhibitor | |
| KRAS G12C inhibitor 47 | Pan Inhibitor | |
| KRAS inhibitor-15 | Pan Inhibitor | |
| KRAS G12C inhibitor 48 | Pan Inhibitor | |
| KRAS inhibitor-18 | Pan Inhibitor | |
| KRAS G12C inhibitor 55 | Pan Inhibitor | |
| KRAS G12C inhibitor 51 | Pan Inhibitor | |
| KRAS G12C inhibitor 54 | Pan Inhibitor | |
| KRAS inhibitor-17 | Pan Inhibitor | |
| SOS1-IN-6 | Pan Inhibitor | |
| SAH-SOS1A | Pan Inhibitor | |
| KRAS G12C inhibitor 53 | Pan Inhibitor | |
| KRAS inhibitor-3 | Inhibitor | 99.65% |
| RM-018 | Inhibitor | 98.03% |
| Garsorasib | Inhibitor | 99.11% |
| Atrovastatin-PEG3-FITC | Inhibitor | 98.17% |
| RMC-6291 | Inhibitor | |
| KRAS G12C inhibitor 44 | Inhibitor | |
| KRAS G12C inhibitor 46 | Inhibitor | |
| Sotorasib-d7 | Inhibitor | |
| CFL-137 | Inhibitor | 99.53% |
| TUS-007 | Degrader | |
| K-Ras(G12C) inhibitor 6 | Inhibitor | |
| KRAS G12D inhibitor 17 | Inhibitor | |
| KRAS G12C inhibitor 43 | Inhibitor | |
| PROTAC SOS1 degrader-2 | Inhibitor | |
| CFL-120 | Inhibitor | ≥98.0% |
| KRAS G12C inhibitor 45 | Inhibitor | |
| ZG1077 | Inhibitor |