Product Details
| Product Name:
Sotorasib |
CAS No.:
2296729-00-3 |
| Purity:
99.89% |
Supply Ability:
10g |
| Release date:
2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | Sotorasib |
| 描述 | Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors. |
| 體外活性 | METHODS: Twenty-two tumor cells were treated with Sotorasib (0-10 μM) for 72 h. Cell viability was measured using the CellTiter-Glo Luminescent Cell Viability Assay kit.
RESULTS: Sotorasib impaired the growth of all KRAS G12C cell lines except SW1573, with IC50 values ranging from 0.004-0.032 μM. non-KRAS G12C cell lines were sensitive to Sotorasib, with an IC50 >7.5 μM. [1]
METHODS: KRAS G12C mutant tumor cells were treated with Sotorasib (100 nM) for 4-72 h, and the expression levels of target proteins were detected using Western Blot method.
RESULTS: Sotorasib rapidly inhibited KRAS downstream signaling, but p-ERK levels returned to 75% of the baseline level at 72 h. Sotorasib was also shown to rapidly inhibit KRAS downstream signaling. [2] |
| 體內(nèi)活性 | METHODS: To assay antitumor activity in vivo, Sotorasib (3-100 mg/kg) was orally administered once daily for four weeks to athymic nude mice bearing the human pancreatic cancer tumor MIA PaCa-2 T2 or the human lung cancer tumor NCI-H358.
RESULTS: Sotorasib significantly inhibited the growth of MIA PaCa-2 T2 and NCI-H358 tumors at all doses, and tumor regression was observed at higher doses. [1]
METHODS: To assay antitumor activity in vivo, Sotorasib (30 mg/kg in 0.5% sodium carboxymethylcellulose, administered by gavage once daily) and Cisplatin (4 mg/kg in 0.9% saline, intraperitoneally every two days) were administered to Balb/C nude mice harboring human lung cancer tumors.
RESULTS: Tumor shrinkage in the combination group was more than twice that of the single-administration group. [3] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : 33.33 mg/mL (59.46 mM), when pH is adjusted to 11 with NaOH. Sonication is recommended.
DMSO : 60 mg/mL (107.03 mM), Sonication is recommended.
|
| 關(guān)鍵字 | Ras | AMG510 | KRAS | covalent | regression | mutation | Inhibitor | G12C | anti-tumour | inhibit | Sotorasib | GDP-bound | AMG 510 | phosphorylation | NSCLC |
| 相關(guān)產(chǎn)品 | Adagrasib | (S)-AMG-510 | BI-2493 | CCG-257081 | Ketoconazole | Deltarasin | ZCL278 | MRTX1133 | Salirasib | RMC-6236 | (S)-(-)-Perillyl alcohol | CASIN |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 疼痛相關(guān)化合物庫(kù) | 膜蛋白靶向化合物庫(kù) | 激酶抑制劑庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌上市藥物庫(kù) | FDA 上市激酶抑制劑庫(kù) | FDA 上市藥物庫(kù) | GPCR靶點(diǎn)分子庫(kù) | 抗癌活性化合物庫(kù) |
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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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States