Taletrectinib free base NEW
| Price | $65 | $159 | $255 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: Taletrectinib free base | CAS No.: 1505514-27-1 |
| Purity: 99.87% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Taletrectinib free base |
| 描述 | Taletrectinib free base (AB-106 free base) is a novel potent, selective and orally active ROS1/NTRK inhibitor.Taletrectinib free base has potent inhibitory effects on recombinant ROS1, NTRK1, NTRK2, and NTRK3, with IC50s of 0.207, 0.622, 2.28 and 0.98 nM, respectively, Taletrectinib free base also inhibited ROS1 G2032R and other Crizotinib-resistant ROS1 mutations. |
| 體外活性 | Taletrectinib free base (1-1000 nM; 72 h) has an IC50 of ~3 -20 nM against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells.[1] Taletrectinib free base (0.001-1000 nM; 2 h) dose-dependently inhibits ROS1 autophosphorylation in U-118-MG cells in vitro.[1] Taletrectinib free base potently inhibits ROS1 autophosphorylation in JFCR-165, JFCR-168 and MGH193-1B cells.[1] Taletrectinib free base partially inhibits phosphorylated NTRK1 at 10 nM and completely inhibits it at 100 nM. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 in an ATP-competitive manner at subnanomolar concentrations. Taletrectinib free base at 0.2 μM almost completely inhibits ACK, ALK, DDR1, and LTK among the 160 kinases but does not strongly inhibit the other 152 kinases in the presence of 1 mM ATP.[1] Taletrectinib free base effectively inhibits crizotinib-resistant ROS1 secondary mutations, including the G2032R solvent front mutation.[1] |
| 體內(nèi)活性 | Taletrectinib free base (DS-6051b) (25 - 200 mg/kg; oral; once daily for 18 days) demonstrates anti-tumor activity in Balb-c nu/nu mice bearing U-118 MG cells. Taletrectinib free base (6.25 - 200 mg/kg; oral; once daily for 8 days) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice harboring KM12 cells. Taletrectinib free base (3 - 100 mg/kg; p.o.; once daily for 4 days) induces rapid tumor regression in wild-type (WT) and G2032R mutant Ba/F3-carrying mice without severe weight loss.[1] |
| 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 : 55 mg/mL (135.65 mM) |
| 關(guān)鍵字 | DS-6051b | IBI 344 | IBI-344 | Taletrectinib | IBI344 |
| 相關(guān)產(chǎn)品 | Lorlatinib | Entrectinib | ROS kinases-IN-1 | Crizotinib hydrochloride | Iruplinalkib | Uniconazole | Crizotinib | Merestinib | ROS kinases-IN-2 | ROS-generating?agent?1 |
| 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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