Home Angiogenesis HIF modulator FG-2216 For research use only.

FG-2216

FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2.

FG-2216 Chemical Structure

FG-2216 Chemical Structure

CAS: 223387-75-5

Selleck's FG-2216 has been cited by 2 publications

Purity & Quality Control

Batch: S797901 DMSO] 56 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.78%
99.78

FG-2216 Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

Choose Selective HIF Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hep3B cells Function assay Inhibition of PHD2 in human Hep3B cells assessed as erythropoietin secretion by ELISA, IC50=3.9 μM 24894560
Hep3B cells Function assay 100 uM 24 h Inhibition of PHD2 in human Hep3B cells assessed as increase in erythropoietin secretion at 100 uM after 24 hrs by ELISA 24894560
HEK293 cells Function assay Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin, IC50=3.5 nM 23844574
Click to View More Cell Line Experimental Data

Biological Activity

Description FG-2216 is a potent, and orally active HIF prolyl 4-hydroxylase inhibitor with IC50 of 3.9 μM for PHD2. Phase 2.
Targets
PHD2 [1]
(Cell-free assay)
3.9 μM
In vitro
In vitro FG-2216 shows the ability to stabilize HIF-α to stimulate EPO secretion. [1]
In Vivo
In vivo In male rhesus macaques, FG-2216 (60 mg/kg, p.o.), induces significant and reversible Epo induction, and induces a small elevation of HbF expression. [2]
Animal Research Animal Models Male rhesus macaques
Dosages 60 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 280.66 Formula

C12H9ClN2O4
CAS No. 223387-75-5 SDF Download FG-2216 SDF
Smiles C1=CC=C2C(=C1)C(=C(N=C2Cl)C(=O)NCC(=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 56 mg/mL ( (199.52 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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