KIF18A-IN-6 (Compound 134) is an orally bioactive KIF18A inhibitor that can suppress KIF18A microtubule-dependent ATPase activity with IC50 of 0.016 μM.

Physicochemical Properties

Molecular Formula	C28H37N3O5S2
Molecular Weight	559.740484952927
Exact Mass	559.217
CAS #	2914879-10-8
PubChem CID	167493856
Appearance	White to off-white solid powder
LogP	4.6
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	7
Heavy Atom Count	38
Complexity	1100
Defined Atom Stereocenter Count	0
InChi Key	AXRRVVWONHGXHG-UHFFFAOYSA-N
InChi Code	InChI=1S/C28H37N3O5S2/c1-5-37(33,34)29-21-9-10-24-23(18-21)28(15-13-27(11-12-27)14-16-28)19-31(24)25(32)20-7-6-8-22(17-20)38(35,36)30-26(2,3)4/h6-10,17-18,29-30H,5,11-16,19H2,1-4H3
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	IC50: 0.016 μM (KIF18A microtubule-dependent ATPase activity)[1]
ln Vitro	KIF18A-IN-6 (Compound 134; 7 days) has an IC50 of 0.0040, 0.0051, and 0.0051 μM, respectively, which decreases the viability of JIMT-1, HCC-15, and NIH-OVCAR3 cells[1].
ln Vivo	KIF18A-IN-6 (Compound 134) (10–60 mg/kg; po; twice or once daily for one month) suppresses the formation of HCC15 and OVCAR3 tumors in mice [1].
Cell Assay	Cell Viability Assay[1] Cell Types: HCC-15, JIMT-1 and NIH-OVCAR3 Tested Concentrations: Incubation Duration: 7 days Experimental Results: Inhibited cell viability with IC50s of 0.0040, 0.0051 and 0.0051 μM against JIMT-1, HCC-15 and NIH-OVCAR3 cells, respectively.
Animal Protocol	Animal/Disease Models: SCID Beige mice, HCC15 tumor model[1] Doses: 10, 30 and 60 mg/kg Route of Administration: PO, twice a day for 1 month Experimental Results: Inhibited tumor growth by 61±10%, 89±7% and 94±5% at 10, 30 and 60 mg/kg, respectively. Animal/Disease Models: Balb/C nude mice, OVCAR3 tumor model[1] Doses: 10 , 30 and 60 mg/kg Route of Administration: PO, twice or one time/day for 1 month Experimental Results: Completely inhibited tumor growth (over 100%) over 30 mg/kg.
References	[1]. SPIRO INDOLINE INHIBITORS OF KIF18A. Patent WO2023028564.

Solubility Data

Solubility (In Vitro)

DMSO : 125 mg/mL (223.32 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (3.72 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 20.8 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	1.7865 mL	8.9327 mL	17.8654 mL
	5 mM	0.3573 mL	1.7865 mL	3.5731 mL
	10 mM	0.1787 mL	0.8933 mL	1.7865 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.