IK-930 (compound I-32) is a potent orally bioactive TEAD inhibitor (antagonist) with EC50 <0.1 µM.

Physicochemical Properties

Molecular Formula	C19H19F3N4O2S
Molecular Weight	424.439973115921
Exact Mass	424.118
CAS #	2563892-44-2
PubChem CID	155342988
Appearance	White to off-white solid powder
LogP	3
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	6
Heavy Atom Count	29
Complexity	632
Defined Atom Stereocenter Count	0
InChi Key	TVBGCXJDLVRDSU-UHFFFAOYSA-N
InChi Code	InChI=1S/C19H19F3N4O2S/c1-23-29(27,28)15-7-8-17(16(9-15)18-11-26(2)12-25-18)24-10-13-3-5-14(6-4-13)19(20,21)22/h3-9,11-12,23-24H,10H2,1-2H3
Chemical Name	N-methyl-3-(1-methylimidazol-4-yl)-4-[[4-(trifluoromethyl)phenyl]methylamino]benzenesulfonamide
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	TEAD[1]
ln Vivo	IK-930 (compound I-32) (10 mg/kg; po) in BALB/c mice shows favorable pharmacokinetic characteristics, with an AUC 0-last of 4581 ng*h /mL and a Cmax of 1088 ng/mL[1].
References	[1]. Tead inhibitors and uses thereof. WO2020243415A2.
Additional Infomation	IK-930 is an oral, paralog-selective TEAD inhibitor.

Solubility Data

Solubility (In Vitro)

DMSO: 100 mg/mL (235.60 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3560 mL	11.7802 mL	23.5605 mL
	5 mM	0.4712 mL	2.3560 mL	4.7121 mL
	10 mM	0.2356 mL	1.1780 mL	2.3560 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.