Name: FG-2216
Brand: Selleck Chemicals
SKU: S7979
Availability: InStock
Rating: 5 (3 reviews)

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.78

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src FLT FLT3 HER2 Bcr-Abl
Other HIF Inhibitors	PT2399 PX-478 Dihydrochloride BAY 87-2243 KC7F2 Lificiguat (YC-1) IOX2 CAY10585 (LW 6) PT2385 Molidustat (BAY 85-3934) IDF-11774

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
Hep3B cells	Function assay			Inhibition of PHD2 in human Hep3B cells assessed as erythropoietin secretion by ELISA, IC50=3.9 μM
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
HEK293 cells	Function assay			Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin, IC50=3.5 nM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (199.52 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2% DMSO 1 40% PEG 300 2 2% Twenn 80 3 ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (2.14mM)	Taking the 1 mL working solution as an example, add 20 μL of 30 mg/ml clear DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween-80 to the above system, mix evenly to clarify it; Then continue to add 560 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	280.66	Formula	C₁₂H₉ClN₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	223387-75-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C2C(=C1)C(=C(N=C2Cl)C(=O)NCC(=O)O)O

Mechanism of Action

Targets/IC₅₀/Ki	PHD2 (Cell-free assay) 3.9 μM
In vitro	FG-2216 shows the ability to stabilize HIF-α to stimulate EPO secretion.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24042008/ [2] https://pubmed.ncbi.nlm.nih.gov/17557894/

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FG-2216 HIF modulator

Chemical Structure

Molecular Weight: 280.66