Zoligratinib NEW
| Price | $39 | $72 | $126 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: Zoligratinib | CAS No.: 1265229-25-1 |
| Purity: 98.94% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Zoligratinib |
| 描述 | Zoligratinib (CH5183284) is a selective and orally available FGFR inhibitor, which is for FGFR1(IC50=9.3 nM), FGFR2(IC50=7.6 nM), FGFR3(IC50=290), and FGFR4(IC50=22 nM), respectively. |
| 細(xì)胞實(shí)驗(yàn) | The cell lines are added to the wells of 96-well plates containing 0.076 to 10,000 nM CH5183284/Debio 1347 and incubated at 37°C. After 4 days of incubation, Cell Counting Kit-8 solution is added and, after incubation for several more hours, absorbance at 450 nm is measured with the iMark Microplate-Reader. The antiproliferative activity is calculated using the formula (1 ? T/C) × 100 (%), where T and C represent absorbance at 450 nm of the cells treated with drugs (T) and that of untreated control cells (C). The IC50 values are calculated using Microsoft Excel 2007.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Protein kinase assay: The inhibitory activity of CH5183284/Debio 1347 against FGFR1 is evaluated using a radiometric filter assay by measuring the incorporation of 33Pi with a microplate scintillation counter. The phosphorylation activities of LCK, EGFR, KIT, MET, SRC, BRK, FGFR2, Flt3, LTK, INSR, YES, ABL, EPHA2, ZAP70, Fyn, IGF1R, KDR, and PDGFR on substrate peptides are determined by homogeneous time-resolved fluorescence assay with LANCE Eu-W1024 labeled anti-phosphotyrosine PT66 antibody according to standard methods. Time-resolved fluorescence is measured with an EnVision HTS microplate reader. The activities of Aurora A, Akt1/PKBα, PKA, Cdk1/cyclin B, Cdk2/cyclin A, PKCα, PKCβ1 and PKCβ2 on substrate peptides are determined by IMAP FP Screening Express Progressive Binding System. Fluorescence polarization is measured with an EnVision HTS microplate reader. |
| 體外活性 | In the DMS114 (FGFR1 amplification), SNU-16 (FGFR2 amplification), and KMS11 cell lines,CH5183284(100 to 300 nM) prevents autophosphorylation of FGFR1, FGFR2, and FGFR3. |
| 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 (2.8 mM), Heating is recommended. DMSO : 66 mg/mL (185.2 mM) |
| 關(guān)鍵字 | Debio1347 | Fibroblast growth factor receptor | CH 5183284 | FF-284 | Inhibitor | Debio-1347 | inhibit | CH-5183284 | FGFR | Zoligratinib | FF 284 |
| 相關(guān)產(chǎn)品 | Amlexanox | Nintedanib | Pazopanib Hydrochloride | Ferulic Acid | Nintedanib esylate | Ponatinib | Pemigatinib | Formononetin | Lenvatinib mesylate | Erdafitinib | Lenvatinib | Pazopanib |
| 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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