KRAS-G12C 抑制劑-Daraxonrasib (RMC-6236) | CAS# 2765081-21-6 Selleck貨號 E1597
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Daraxonrasib (RMC-6236) 是一種RAS(ON)多選擇性非共價抑制劑，可抑制經典 RAS 亞型突變體和野生型的活性 GTP 結合狀態，具有廣泛的治療潛力。 RMC-6236 在 RAS 依賴性細胞株中表現出強大的抗癌功效，尤其對 KRAS 12 號密碼子突變的細胞株效果顯著。
KRAS-G12C 抑制劑-Daraxonrasib (RMC-6236) | CAS# 2765081-21-6 Selleck貨號 E1597
Daraxonrasib is a potent pan-KRAS inhibitor. It affects RAS signaling by targeting RAS(ON), inhibiting cell viability.
產品介紹
Daraxonrasib (RMC-6236) 是一種RAS(ON)多選擇性非共價抑制劑，可抑制經典 RAS 亞型突變體和野生型的活性 GTP 結合狀態，具有廣泛的治療潛力。 RMC-6236 在 RAS 依賴性細胞株中表現出強大的抗癌功效，尤其對 KRAS 12 號密碼子突變的細胞株效果顯著。胰腺導管腺癌 (PDAC)Daraxonrasib (RMC-6236) 在攜帶 RAS 突變且先前接受過治療的轉移性胰腺導管腺癌患者中，展現出了前所未有的總生存期 (OS) 和無進展生存期 (PFS) 獲益。包括 RASolute 302 在內的近期 3 期臨床試驗表明，該藥物顯著優於標準的細胞毒性化療。作為首款同類（first-in-class）口服 RAS(ON) 多重選擇性抑制劑，它能有效靶向突變型及野生型 RAS 蛋白。這項突破性進展解決了針對這種高致死性惡性腫瘤的一項關鍵未滿足醫療需求，從而引發了廣泛的科學關注，並有望在全球範圍內獲得快速監管批准。在非小細胞肺癌 (NSCLC)中，Daraxonrasib 的研究主要集中在攜帶特定 RAS 突變且先前接受過標準治療後病情進展的非小細胞肺癌患者。包括 RASolve 301 研究在內的全球 III 期臨床試驗正在積極評估其療效、安全性和藥物動力學，並與多西他賽等標準療法進行比較。作為一種強效的泛 RAS 分子膠抑制劑，Daraxonrasib 旨在透過廣泛靶向 RAS 同工酶的活性狀態來克服現有突變特異性抑制劑的局限性，從而為這種常見且棘手的癌症類型提供一種備受期待的靶向治療選擇。大腸直腸癌 (CRC) 達拉西布 (Daraxonrasib) 正被廣泛研究，作為一種有前景的標靶治療手段，用於治療攜帶多種致癌 RAS 突變的轉移性或不可切除的結直腸癌。目前正在進行的早期臨床試驗和聯合臨床試驗正在嚴格評估其安全性、耐受性和初步抗腫瘤活性。由於 RAS 突變在結直腸癌中普遍存在，並且通常會導致對傳統標靶療法的抗藥性，這種新型多選擇性 RAS(ON) 抑制劑提供了一種重要的全新治療策略。研究人員尤其關注其誘導深度分子反應的潛力，以及其與胃腸道惡性腫瘤中的其他抗腫瘤藥物聯合使用時的協同效應。
| Storage | |
| M.Wt | 811.05 |
| Cas No. | 2765081-21-6 |
| Formula | C44H58N8O5S |
| Synonyms | RMC-6236; RAS-IN-2 |
| Solubility | DMSO : 100 mg/mL (123.29 mM) (Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)Ethanol : 100 mg/mLWater : Insoluble |
| 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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