KRAS G12C 抑制劑-Adagrasib (MRTX849) | CAS# 2326521-71-3 Selleck貨號 S8884
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Adagrasib (MRTX849) 是一種強效、選擇性的共價 KRAS G12C 抑制劑。它透過與突變型 KRAS 蛋白的 Cys12 位點共價結合，影響 KRAS/MAPK/ERK 訊號通路，從而有效抑制 KRAS 依賴性訊號傳導，並抑制癌細胞的活力與增殖。
KRAS G12C 抑制劑-Adagrasib (MRTX849) | CAS# 2326521-71-3 Selleck貨號 S8884
Adagrasib (MRTX849) is a potent, selective, and covalent KRAS G12C inhibitor. It affects the KRAS/MAPK/ERK signaling pathways by covalently binding to the mutant KRAS protein at Cys12, effectively inhibiting KRAS-dependent signal transduction and suppressing cancer cell viability and proliferation.
產品介紹
非小細胞肺癌：Adagrasib (MRTX849) 徹底改變了攜帶KRAS G12C突變的非小細胞肺癌的治療模式。大量臨床試驗已證實，無論作為單藥治療或與免疫檢查點抑制劑（如帕博利珠單抗）聯合治療，Adagrasib (MRTX849) 均具有顯著療效和良好的安全性。研究人員正在積極探索其穿透血腦屏障的能力，以治療中樞神經系統轉移——這是晚期肺癌常見的併發症。目前的研究旨在將Adagrasib (MRTX849) 確立為第一線治療方案，從而顯著提高攜帶該特定基因突變患者的無惡化存活期和總存活期。在大腸直腸癌領域，Adagrasib (MRTX849) 展現出令人鼓舞的臨床活性，尤其是在聯合治療中。由於大腸直腸腫瘤常透過表皮生長因子受體（EGFR）訊號路徑的重新活化而對KRAS抑制劑產生抗藥性，因此Adagrasib (MRTX849) 與西妥昔單抗（cetuximab）的聯合治療已成為主要的研究方向。這種協同療法在先前接受過大量治療的患者中取得了較高的客觀緩解率和長期的疾病控制。近期監管機構對此聯合療法的批准進一步推動了克服適應性抗藥性機制和優化晚期大腸直腸癌治療順序的研究。除了肺癌和大腸直腸癌之外，Adagrasib (MRTX849) 在胰腺導管腺癌和其他攜帶KRAS G12C突變的胃腸道腫瘤中的治療潛力也正在被廣泛評估。這些癌症以往被認為無法成藥，預後極差，但在早期臨床試驗中，Adagrasib (MRTX849) 單藥治療顯示出令人鼓舞的客觀緩解率。目前，研究人員正致力於擴大這些隊列，以更好地了解療效的持久性和安全性。此外，研究也正在探索合理的合併用藥策略，以提高療效並延緩這些高度侵襲性實體腫瘤獲得性抗藥性的發生。
| Product Name | Key Target | IC50 | Applications | Strengths | Limitations |
| Daraxonrasib (RMC-6236) | pan-RAS / RAS(ON) | — | Treatment of patients with multiple RAS-addicted cancers, including pancreatic ductal adenocarcinoma (PDAC) and non-small cell lung cancer (NSCLC). | Broad-spectrum RAS inhibition with generally controllable side effects and effective tolerance by most patients. | The potential for broad RAS inhibition to disrupt normal tissue homeostasis remains a significant concern. |
| AMG 510 (Sotorasib) | KRAS G12C | — | Treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with KRAS G12C mutation. | First G12C inhibitor to enter and complete clinical trials. Its binding induces an alternative orientation of His-95, providing a novel surface groove that enhances interaction and improves potency, exhibiting a 10-fold increase in efficacy compared to AR | Preclinical studies showed potential for renal toxicity at high doses and poor brain distribution. |
| Lonafarnib (SCH66336) | Farnesyltransferase (FTase) | 1.9 nM | Reduction of mortality risk in Hutchinson-Gilford Progeria Syndrome (HGPS) and treatment of processing-deficient progeroid laminopathies. | First approved therapy for reducing mortality risk in HGPS. It is a nonpeptidic, CAAX-competitive, selective FTase inhibitor. | Development for oncology was discontinued due to lack of efficacy, and it has a high incidence of gastrointestinal adverse events. |
| Adagrasib (MRTX849) | KRAS G12C | 5 nM | Treatment of advanced or metastatic solid tumors harboring a KRAS G12C mutation, such as NSCLC and colorectal cancer. | High oral bioavailability, long half-life (>50 hours), extensive tissue distribution, and central nervous system penetration. It has >1000-fold selectivity for KRAS G12C over wild-type KRAS. | Common treatment-related adverse events include nausea, diarrhea, vomiting, fatigue, and increased ALT. |
KRas 抑制劑
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