Product Details
| Product Name:
ASTX660 |
CAS No.:
1799328-86-1 |
| Purity:
98.33% |
Supply Ability:
10g |
| Release date:
2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | ASTX660 |
| 描述 | Tolinapant (ASTX660) is an orally bioavailable cIAP1/2 and XIAP antagonist that induces expression of immunogenic cell death (ICD) markers in sensitive HNSCC cell lines in vitro. |
| 體外活性 | METHODS: Four human HNSCC cell lines (3 HPV-, 1 HPV+) were treated with IFN-γ (positive control, 10 ng/mL), TNFα (20 ng/mL), Tolinapant (ASTX660) (500 nM, 1 μM), and ASTX660 (250 nM, 500 nM, 1 μM) + TNFα for 48 hours, and then the intracellular APM components were analyzed by flow cytometry.
RESULTS In all four cell lines, HLA-A, B, and C expression was consistently increased under ASTX660 + TNFα treatment. ASTX660 + TNFα may enhance tumor cell killing. [1]
METHODS: DLD1, HCT116, and SW48 were treated with ASTX660 (0.04, 0.2, 1 μM, 24 hours). After washing and cell lysis, western blot analysis was performed using antibodies specific for the indicated proteins.
RESULTS ASTX660 concentrations as low as 40 nM were sufficient to rapidly reduce cIAP2 (but not cIAP1) levels. [2] |
| 體內(nèi)活性 | METHODS: Tolinapant (ASTX660)(16 mg/kg, oral), XRT (single dose 8 Gy), or a combination of both treated a MEER syngeneic tumor xenograft mouse model. Tumors, spleens, and DLNs were harvested and analyzed for CD8 lymphocytes by flow cytometry. Tumor subpopulations were digested and T cells were magnetically selected and cocultured with inactivated dendritic cells presenting p15E peptide. Subsequent IFN-γ production was quantified using an ELISpot assay.
RESULTS The number of CD8+ T cells in the spleen was significantly increased in animals treated with ASTX660 alone and in the subpopulation of animals treated with radiation ± ASTX660 (Figure 3(b)). In the draining lymph nodes of animals treated with XRT alone There was a significant increase in the number of CD8 T lymphocytes and an almost significant increase in the number of CD8 T lymphocytes in animals that received the combination treatment. [1] |
| 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 | DMSO : 47 mg/mL (87.09 mM)
|
| 關(guān)鍵字 | ASTX660 | ASTX-660 | Inhibitor | inhibit | IAP | ASTX 660 |
| 相關(guān)產(chǎn)品 | LCL161 | MX69 | Se-Methylselenocysteine | HM90822 | BV6 | 1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one | AZD5582 TFA | N-Deshydroxyethyl Dasatinib | Xevinapant | GDC-0152 | Acacetin | Birinapant |
| 相關(guān)庫(kù) | 細(xì)胞凋亡化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 血液病分子庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌藥物庫(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 |
|
|
$0.00/100MG |
VIP1Y
|
Hubei Chuchang Biotech Co., Ltd.
|
2024-04-17 |
United States