Amuvatinib NEW
| Price | $44 | $62 | $93 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: Amuvatinib | CAS No.: 850879-09-3 |
| Purity: 99.54% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Amuvatinib |
| 描述 | Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity. |
| 細胞實驗 | Cells are plated at a density of 2 × 103 to 1 × 104 cells per well in 100 μL medium on day 0 in 96-well Falcon microtitier plates. On day 1, ten μL of serial dilutions of MP-470 are added to the plates in quadruplicates. After incubation for 4 days, the cells are fixed with 10% Trichloroacetic acid solution. Subsequently, they are labeled with 0.04% Sulforhodamine B (SRB) in 1% acetic acid. After multiple washes to remove the excess dye, 100 μL of 50 mM Tris solution is added to each well in order to dissolve the dye. The absorbance of each well is read on a plate reader at 570 nm. Date are expressed as the percentage of survival of control calculated from the absorbance corrected for background absorbance. The surviving percent of cells is determined by dividing the mean absorbance values of the monoclonal antibody by mean absorbance values of the control and multiplying by 100.(Only for Reference) |
| 激酶實驗 | Kinase inhibition assay of c-Kit and PDGFRα: For the testing of inhibitory activity against c-Kit and PDGFRα, enzymes are incubated with varying concentrations of MP-470 and radiolabeled γ-32P-ATP. After 30 min, the reaction mixtures are electrophoresed on an acrylamide gel and autophosphorylation, quantitated by the amount of radioactivity incorporated into the enzyme, is assayed. |
| 體外活性 | Tumor growth was inhibited by intraperitoneal injection of 10 mg/kg-75 mg/kg or by oral administration of 50 mg/kg-200 mg/kg MP-470 in a mouse transplantation tumor model harboring HT-29, A549, and SB-CL2 cells.The combination of 20 mg/kg MP-470 and erlotinib markedly inhibited the tumor growth in mice harboring LNCaP transplantation tumors. tumor growth in mice bearing LNCaP graft tumors. |
| 體內(nèi)活性 | 1 μM MP-470 inhibited tyrosine phosphorylation of AXL in MDA-MB-231 cells.10 μM MP-470 caused cell cycle arrest in the G1 phase and decreased Akt and ERK1/2 phosphorylation in LNCaP cells.10 μM MP-470 inhibited c-Met phosphorylation in SF767 cells and sensitized the cells to radiation.10 μM MP-470 combined with radiation inhibited GSK-3β activity, induced apoptosis, and disrupted dsDNA b break repair, possibly by inhibiting Rad51. 470 inhibited GSK-3β activity and induced apoptosis in combination with radiation, and disrupted dsDNA b-break repair, possibly by inhibiting Rad51. MP-470 hydrochloride effectively inhibited the proliferation of OVCAR-3, A549, NCI-H647, DMS-153, and DMS-114 cells, with an IC50 of 0.9 μM to 7.86 μM. 7.86 μM. MP-470 was toxic to MiaPaCa-2, PANC-1 and GIST882 cells with IC50s ranging from 1.6 μM to 3.0 μM. MP-470 was toxic to LNCaP and PC-3 but not to DU145 cells with IC50s of 4 μM and 8 μM, respectively, and induced apoptosis at 10 μM. |
| 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 : 1 mg/ml, Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
| 關鍵字 | HPK56 | c-Kit | MP 470 | MP-470 | HPK-56 | c-Met/HGFR | Apoptosis | Fms like tyrosine kinase 3 | Cluster of differentiation antigen 135 | RET | FLT3 | CD117 | CD135 | Platelet-derived growth factor receptor | PDGFR | SCFR | Amuvatinib | Inhibitor | RAD51 | inhibit |
| 相關產(chǎn)品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Guanidine hydrochloride | Metronidazole | Sorafenib | Tributyrin | Thymidine |
| 相關庫 | 經(jīng)典已知活性庫 | 膜蛋白靶向化合物庫 | 酪氨酸激酶分子庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 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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