Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
Other Sizes |
|
Targets |
IC50: 9.4 nM (KIF18A microtubule-dependent ATPase activity)[1]
|
---|---|
ln Vitro |
KIF18A-IN-7 (Compound 22; 7 days) has an IC50 of 0.0078, 0.0097, and 0.011 μM, respectively, that reduces the viability of JIMT-1, NIH-OVCAR3, and HCC-15 cells [1].
|
ln Vivo |
KIF18A-IN-7 (Compound 22) suppresses the formation of HCC15 and OVCAR3 tumors in mice when given orally twice or thrice a day for a month (10–60 mg/kg) [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 0.0078, 0.0097 and 0.011 μM against JIMT-1, NIH-OVCAR3 and HCC-15 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 30±15%, 72±6% and 82±9% 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, one time/day for 1 month Experimental Results: Inhibited tumor growth by 24±26%, 72±17% and 82±10% at 10, 30 and 60 mg/kg, respectively. |
References |
[1]. COGAN, et al. SPIRO INDOLINE INHIBITORS OF KIF18A. Patent WO2023028564.
|
Molecular Formula |
C27H35N3O5S2
|
---|---|
Molecular Weight |
545.71
|
CAS # |
2914878-00-3
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
C(C1C=CC=C(C=1)S(=O)(=O)NC(C)(C)C)(N1C2=CC=C(C=C2C2(CCC3(CC3)CC2)C1)NS(=O)(=O)C)=O
|
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)
|
Solubility (In Vitro) |
DMSO : 25 mg/mL (45.81 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.58 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 | 1.8325 mL | 9.1624 mL | 18.3248 mL | |
5 mM | 0.3665 mL | 1.8325 mL | 3.6650 mL | |
10 mM | 0.1832 mL | 0.9162 mL | 1.8325 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.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.