Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
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5 mg | 在庫あり | ¥ 9,000 | |||
10 mg | 在庫あり | ¥ 16,500 | |||
25 mg | 在庫あり | ¥ 29,000 | |||
50 mg | 在庫あり | ¥ 45,500 | |||
100 mg | 在庫あり | ¥ 85,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 10,000 |
説明 | 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. |
ターゲット&IC50 | FGFR4:290 nM, FGFR3:22 nM, FGFR1:9.3 nM, FGFR2:7.6 nM |
In vitro | 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. |
キナーゼ試験 | 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. |
細胞研究 | 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) |
別名 | FF284, CH5183284, Debio 1347 |
分子量 | 356.38 |
分子式 | C20H16N6O |
CAS No. | 1265229-25-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 1 mg/mL (2.8 mM), Heating is recommended.
DMSO: 66 mg/mL (185.2 mM)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Zoligratinib 1265229-25-1 Angiogenesis Tyrosine Kinase/Adaptors FGFR Debio1347 Fibroblast growth factor receptor CH 5183284 FF-284 FF284 Inhibitor CH5183284 Debio-1347 inhibit CH-5183284 Debio 1347 FF 284 inhibitor