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Cat.No.S7714
| Related Targets | EGFR VEGFR PDGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit |
|---|---|
| Other FGFR Products | PD173074 Fexagratinib (AZD4547) BLU9931 LY2874455 Zoligratinib (Debio-1347) Futibatinib (TAS-120) PD-166866 SSR128129E H3B-6527 Fisogatinib (BLU-554) |
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In vitro |
DMSO
: 69 mg/mL
(108.7 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 634.73 | Formula | C35H38N8O4 |
Storage (From the date of receipt) | |
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| CAS No. | 1633044-56-0 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C4CN(C(=O)N(C4=N3)CC5=CC=C(C=C5)NC(=O)C=C)C6=CC(=CC(=C6)OC)OC | ||
| Targets/IC50/Ki |
FGFR1
(Cell-free assay) 3.09 nM
FGFR2
(Cell-free assay) 4.3 nM
FGFR3
(Cell-free assay) 27 nM
FGFR4
(Cell-free assay) 45.3 nM
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| In vitro |
In FGFR1-4 Ba/F3 cells, FIIN-2 inhibits cell proliferation with EC50 in the single- to double-digit nanomolar range. This compound also shows excellent antiproliferative activity in a variety of backgrounds, including cell lines that have gatekeeper mutations in FGFR1 and that are dependent on FGFR4.
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| Kinase Assay |
Biochemical assays
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Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform.
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| In vivo |
In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR.
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References |
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