Product Details
| Product Name:
Tesevatinib |
CAS No.:
781613-23-8 |
| Purity:
97.89% |
Supply Ability:
10g |
| Release date:
2024/11/13 |
Product Introduction
Bioactivity
| 名稱 | Tesevatinib |
| 描述 | Tesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ??of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4. |
| 細(xì)胞實驗 | Growth inhibition of H1975 and A431 cells by increasing concentrations of Tesevatinib is determined by seeding 5000 cells per well in 96-well plates. The following day, cells are washed once with low-serum RPMI 1640 (0.1% fetal bovine serum, 1% nonessential amino acids, and 1% penicillin/streptomycin), after which 90 μL of the low-serum RPMI 1640 is added. Tesevatinib is diluted to 10 times the test concentrations and 10 μL are added to triplicate wells for a 72-h incubation. Cell viability is determined. |
| 動物實驗 | Tumor-bearing mice are given either Tesevatinib, erlotinib, or gefitinib at 100 mg/kg and tumors are harvested 1 to 72 h later. Half an hour before the respective time point, EGF (50 μg/mouse) is given via i.v. bolus injection with tumors dissected 30 min later and tumor extracts are prepared by homogenization in 10 volumes of ice-cold lysis buffer. Lysates are clarified by centrifugation and EGFR tyrosine phosphorylation levels are determined by ELISA. |
| 體外活性 | Tesevatinib (XL-647) potently inhibits the EGF/ErbB2, VEGF, and ephrin RTK families with IC50 values ??of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, and EphB4. [1] |
| 體內(nèi)活性 | METHODS: To study the in vivo effects of Tesevatinib (XL-647) on T790M mutant EGFR, H1975 human tumor xenografts were established in female severe combined immunodeficient mice and administered Tesevatinib (XL-647) orally once daily (doses: 10, 30 and 100 mg/kg, 14 days)
RESULTS Tesevatinib (XL-647) significantly inhibited tumor growth in a dose-dependent manner, with tumor growth inhibition rates of 33%, 66% and 92% respectively.[1]
METHODS: Tesevatinib (XL-647) (7.5, 15 mg/kg, ip, daily) was treated in the well-characterized bpk mouse model of ARPKD, and efficacy and toxicity were evaluated in neonatal mice during postnatal development.
RESULTS In vivo pharmacological inhibition of multiple kinase cascades by tesevatinib (XL-647) reduced phosphorylation of key mediators of cystogenesis: EGFR, ErbB2, c-Src, and KDR; decreased kinase activity resulted in significant reductions in renal and biliary disease in both the bpk and PCK models of ARPKD. Disease amelioration by tesevatinib (XL-647) was not associated with any overt toxicity. [2] |
| 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 : 45 mg/mL (91.58 mM)
|
| 關(guān)鍵字 | EXEL7647 | HER1 | XL647 | Ephrin Receptor | Inhibitor | VEGFR | Vascular endothelial growth factor receptor | KD019 | Epidermal growth factor receptor | KD 019 | EGFR | ErbB-1 | Tesevatinib | XL 647 | EXEL 7647 | inhibit |
| 相關(guān)產(chǎn)品 | Gilteritinib | Osimertinib | Sorafenib | Lapatinib | Regorafenib | Erlotinib hydrochloride | Erlotinib | Neratinib | Genistein | Gefitinib | Pazopanib | Axitinib |
| 相關(guān)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 | 已知活性化合物庫 | 抗癌藥物庫 | 抗癌活性化合物庫 |
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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