| 别名 | RMC 7977; RMC7977; |
| 产品名 | RMC-7977 |
| CAS号 | 2765082-12-8 |
| 目录号 | D700002 |
| 化学式 | C₄₇H₆₀N₈O₆S |
| 分子量 | 865.09 |
| 溶解度 | DMSO 125 mg/mL(144.49 mM) |
| 靶点 | GPCR/G Protein MAPK/ERK Pathway Ras |
| 储存条件 | 3 years -20°C powder |
| 用途 | 仅供科学研究使用!不能用于人体及动物治疗 |
| 纯度 | >98.5% |
靶点及简介 :
RMC-7977 是一种可逆的三复合 RAS 抑制剂,对突变型和野生型 (WT) KRAS、NRAS 和 HRAS 变体均具有广谱活性。RMC-7977 可导致肿瘤消退,并且在多种 RAS成瘾的临床前癌症模型中具有良好的耐受性。RMC-7977 还可以抑制KRASG12C 癌症模型的生长。
In an in vitro study, RMC-7977, a reversible RAS inhibitor, demonstrated potent activity against various RAS-addicted tumors, including those with KRAS codon 12 mutations. 1. Holderfield M, Lee BJ, Jiang J, Tomlinson A, Seamon KJ, Mira A, Patrucco E, Goodhart G, Dilly J, Gindin Y, Dinglasan N, Wang Y, Lai LP, Cai S, Jiang L, Nasholm N, Shifrin N, Blaj C, Shah H, Evans JW, Montazer N, Lai O, Shi J, Ahler E, Quintana E, Chang S, Salvador A, Marquez A, Cregg J, Liu Y, Milin A, Chen A, Ziv TB, Parsons D, Knox JE, Klomp JE, Roth J, Rees M, Ronan M, Cuevas-Navarro A, Hu F, Lito P, Santamaria D, Aguirre AJ, Waters AM, Der CJ, Ambrogio C, Wang Z, Gill AL, Koltun ES, Smith JAM, Wildes D, Singh M. Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy. Nature. 2024 May;629(8013):919-926. doi: 10.1038/s41586-024-07205-6. Epub 2024 Apr 8. PMID: 38589574; PMCID: PMC11111408.
In an in vivo study, RMC-7977, a highly selective inhibitor of active RAS variants, showed significant anti-tumor activity in pancreatic ductal adenocarcinoma (PDAC) models driven by KRAS mutations. 1. Wasko UN, Jiang J, Dalton TC, Curiel-Garcia A, Edwards AC, Wang Y, Lee B, Orlen M, Tian S, Stalnecker CA, Drizyte-Miller K, Menard M, Dilly J, Sastra SA, Palermo CF, Hasselluhn MC, Decker-Farrell AR, Chang S, Jiang L, Wei X, Yang YC, Helland C, Courtney H, Gindin Y, Muonio K, Zhao R, Kemp SB, Clendenin C, Sor R, Vostrejs WP, Hibshman PS, Amparo AM, Hennessey C, Rees MG, Ronan MM, Roth JA, Brodbeck J, Tomassoni L, Bakir B, Socci ND, Herring LE, Barker NK, Wang J, Cleary JM, Wolpin BM, Chabot JA, Kluger MD, Manji GA, Tsai KY, Sekulic M, Lagana SM, Califano A, Quintana E, Wang Z, Smith JAM, Holderfield M, Wildes D, Lowe SW, Badgley MA, Aguirre AJ, Vonderheide RH, Stanger BZ, Baslan T, Der CJ, Singh M, Olive KP. Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer. Nature. 2024 May;629(8013):927-936. doi: 10.1038/s41586-024-07379-z. Epub 2024 Apr 8. PMID: 38588697; PMCID: PMC11111406.
参考文献:
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.16 mL | 5.78 mL | 11.56 mL |
| 5 mM | 0.23 mL | 1.16 mL | 2.31 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.16 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |