SGI-7079 NEW
| Price | $56 | $98 | $198 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-15 |
Product Details
| Product Name: SGI-7079 | CAS No.: 1239875-86-5 |
| Purity: 99.26% | Supply Ability: 10g |
| Release date: 2024/11/15 |
Product Introduction
Bioactivity
| 名稱 | SGI-7079 |
| 描述 | SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance. |
| 細(xì)胞實(shí)驗(yàn) | SGI-7079 show inhibition of Axl activation in HEK-293 cells, which were transiently transfected by electroporation with 1 mg FLAG-tagged plasmid containing the human Axl gene and incubated in standard media + 10% FBS for 24 hours.Cells are treated with SGI-7079( concentrations : 0.03, 0.1, 0.3, 1, 3 μmol/L) for 10 minutes. Five minutes before lysis, the cells are stimulated by WI38 conditioned media containing Gas6. |
| 激酶實(shí)驗(yàn) | In phospho-GEF-H1 cellular assay, TR-293-KDG cells are incubated for 3 hours with PF-3758309. TR-293-KDG cells were captured on an anti-HA antibody-coated plate, which is detected with an anti-phospho-S810-GEF-H1 antibody, and quantified with a horseradish peroxidase-goat anti-rabbit antibody conjugate. TR-293-KDG cells are constructed from HEK293 cells, which is transfected with tetracycline-inducible PAK4-kinase domain (amino acids 291-591) and expressed HA-tagged GEFH1ΔDH (amino acids 210-921). |
| 動(dòng)物實(shí)驗(yàn) | Animal Models: Mouse(NCr-nu/nu female mice) xenograft model of NSCLC using the mesenchymal NSCLC cell line A549Formulation: 0.1N citrate bufferDosages: 10, 25, 50 mg/kgAdministration: p.o. |
| 體外活性 | SGI-7079 exhibits a Ki = 5.7 nM for AXL ,and in HEK293T cells (EC50 = 100 nM) inhibits Gas6 ligand-induced tyrosine phosphorylation of human AXL expressed . Similar to AXL, SGI-7079 inhibits TAM family members such as MER and Tyro3, and shows effective inhibition of Syk, Flt1, Flt3, Jak2, TrkA, TrkB, PDGFRβ and Ret kinases. Mesenchymal cells, which have the increase of the receptor tyrosine kinase Axl, show a trend that has greater sensitivity to the Axl inhibitor SGI-7079. |
| 體內(nèi)活性 | SGI-7079 can be in a dose-dependent manner inhibits tumor growth. And at the maximum dose, 67% tumor can be inhibited growth. Mesenchymal cells showed a trend towards a greater sensitivity to the Axl inhibitor SGI-7079, while the combination of SGI-7079 with erlotinib reversed erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC. |
| 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 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 84 mg/mL (184.4 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 關(guān)鍵字 | Tyro3 | inhibit | Inhibitor | Axl | Mer | TAM Receptor | SGI-7079 | SGI7079 | SGI 7079 |
| 相關(guān)產(chǎn)品 | Gilteritinib | Nintedanib | Regorafenib monohydrate | Sorafenib | Staurosporine | L-Ascorbic acid 2-phosphate trisodium | Pexidartinib | Ibrutinib | Dasatinib | Regorafenib | Sorafenib tosylate | Lenvatinib mesylate |
| 相關(guān)庫(kù) | 抗肺癌化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | HIF-1化合物庫(kù) | 激酶抑制劑庫(kù) | 酪氨酸激酶分子庫(kù) | 抑制劑庫(kù) | 已知活性化合物庫(kù) | 含氟化合物庫(kù) | 抗癌化合物庫(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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