(S)-AMG-510 NEW
| Price | $31 | $48 | $77 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: (S)-AMG-510 | CAS No.: 2252403-56-6 |
| Purity: 98.57% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | (S)-AMG-510 |
| 描述 | (S)-AMG-510 is the S-type compound of AMG-510 (Sotorasib), which effectively and selectively inhibits KRASG12C through covalent interaction with mutant cysteine, thereby promoting clinical efficacy in KRASG12C tumors. |
| 體外活性 | METHODS: KRAS G12 mutant NSCLC cell lines (NCI-H358 [G12C], NCI-H23 [G12C], NCI-H2122 [G12C], A549 [G12S], NCI-H2009 [G12A], NCI-H441 [G12V], and SK-LU1 [G12D]) were treated with (S)-AMG-510 (0.001-100000nM, 72 hours), and cell viability was detected by CCk8. RESULTS All non-G12C cell lines were as expected. Among KRAS G12 C cells, H358 and H2122 were sensitive, but H23 cells were resistant to (S)-AMG-510. METHODS: Engineered Ba/F3 cells carrying KRAS G12C were treated with (S)-AMG-510 (0.001-100000nM, 72 hours), and cell viability was determined by CCK8. RESULTS Ba/F3 cells expressing KRAS G12C were sensitive to sotorasib with an IC50 value of 12.4nM. METHODS: Ba/F3 cells expressing KRAS G12C or G12D were treated with (S)-AMG-510 (10-100nM, 6 hours) or adagrasib and immunoblotted. RESULTS (S)-AMG-510 inhibited pERK and pS6 levels in Ba/F3 cells expressing KRAS G12C; it had no effect on KRAS G12D. [3] |
| 體內(nèi)活性 | METHODS: (S)-AMG-510 (10 mg/kg, oral) or sotorasib (10 mg/kg) + encorafenib (20 mg/kg) were used to treat NOD/SCID mice bearing tumor xenografts. The body weight and tumor size of the mice were monitored every 2 days. RESULTS (S)-AMG-510 withdrawal and the combination of BRAF inhibitors induced tumor regression in vivo. [4] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 5.61 mg/mL (10 mM) |
| 關(guān)鍵字 | Ras | inhibit | AMG 510 | Sotorasib racemate | (S)-Sotorasib | Inhibitor | AMG-510 | Sotorasib | AMG510 |
| 相關(guān)產(chǎn)品 | Adagrasib | BI-2493 | CCG-257081 | Ketoconazole | Deltarasin | ZCL278 | MRTX1133 | Salirasib | RMC-6236 | (S)-(-)-Perillyl alcohol | CASIN | Sotorasib |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 膜蛋白靶向化合物庫 | 抗癌臨床化合物庫 | 抑制劑庫 | 抗癌上市藥物庫 | FDA 上市藥物庫 | 已知活性化合物庫 | GPCR靶點分子庫 | 抗癌活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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