FGFR2-IN-2 (Compound 38) is a selective FGFR2 inhibitor (antagonist) with IC50s of 389, 29 and 758 nM for FGFR1, FGFR2 and FGFR3 respectively.

Physicochemical Properties

Molecular Formula	C23H22N4O
Molecular Weight	370.45
Exact Mass	370.179
CAS #	2677709-81-6
PubChem CID	157049298
Appearance	Light yellow to light brown solid powder
LogP	4
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Heavy Atom Count	28
Complexity	495
Defined Atom Stereocenter Count	0
SMILES	C1(O)=CC=C(C2=CC3=C(C=C2)C(C2=CC=C(N4CCNCC4)C=C2)=NN3)C=C1
InChi Key	OYKIIJTXTXJYKZ-UHFFFAOYSA-N
InChi Code	InChI=1S/C23H22N4O/c28-20-8-3-16(4-9-20)18-5-10-21-22(15-18)25-26-23(21)17-1-6-19(7-2-17)27-13-11-24-12-14-27/h1-10,15,24,28H,11-14H2,(H,25,26)
Chemical Name	4-[3-(4-piperazin-1-ylphenyl)-1H-indazol-6-yl]phenol
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	FGFR2 29 nM (IC50) FGFR1 389 nM (IC50) FGFR3 758 nM (IC50)
References	[1]. From Fragment to Lead: De Novo Design and Development toward a Selective FGFR2 Inhibitor. J Med Chem. 2022 Jan 27;65(2):1481-1504.

Solubility Data

Solubility (In Vitro)

DMSO: 62.5 mg/mL (168.71 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (5.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6994 mL	13.4971 mL	26.9942 mL
	5 mM	0.5399 mL	2.6994 mL	5.3988 mL
	10 mM	0.2699 mL	1.3497 mL	2.6994 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.