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Cat. No.: HY-153065

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KIF18A-IN-6

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KIF18A-IN-6 (Compound 134) is an orally active KIF18A inhibitor with an IC₅₀ of 0.016 μM against KIF18A microtubule-dependent ATPase activity.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 98.48%
CAS No.: 2914879-10-8
Formule: C₂₈H₃₇N₃O₅S₂
Masse moléculaire:559.74

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

KIF18A-IN-6 Chemical Structure

CAS No.: 2914879-10-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

KIF18A-IN-6 (Compound 134) is an orally active KIF18A inhibitor with an IC₅₀ of 0.016 μM against KIF18A microtubule-dependent ATPase activity^[1].

IC₅₀ & Target

IC50: 0.016 μM (KIF18A microtubule-dependent ATPase activity)^[1]

Voir tous les produits spécifiques à Isoform Kinesin :

In Vitro

KIF18A-IN-6 (Compound 134; 7 days) inhibits JIMT-1, HCC-15 and NIH-OVCAR3 cells viability with IC₅₀s of 0.0040, 0.0051 and 0.0051 μM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

HCC-15, JIMT-1 and NIH-OVCAR3
Concentration:
Incubation Time:

7 days
Result:

Inhibited cell viability with IC₅₀s of 0.0040, 0.0051 and 0.0051 μM against JIMT-1, HCC-15 and NIH-OVCAR3 cells, respectively.

In Vivo

KIF18A-IN-6 (Compound 134; 10-60 mg/kg; p.o.; twice or once a day for 1 month) inhibits HCC15 and OVCAR3 tumor growth in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

SCID Beige mice, HCC15 tumor model^[1]
Dosage:

10, 30 and 60 mg/kg
Administration:

PO, twice a day for 1 month
Result:

Inhibited tumor growth by 61±10%, 89±7% and 94±5% at 10, 30 and 60 mg/kg, respectively.

Animal Model:

Balb/C nude mice, OVCAR3 tumor model^[1]
Dosage:

10, 30 and 60 mg/kg
Administration:

PO, twice or once a day for 1 month
Result:

Completely inhibited tumor growth (over 100%) over 30 mg/kg.

Chemical Information

CAS No. 2914879-10-8
Appearance Solid
Masse moléculaire 559.74
Formule C₂₈H₃₇N₃O₅S₂
Color White to off-white
SMILES

O=S(C1=CC(C(N2CC3(CCC4(CC4)CC3)C5=CC(NS(CC)(=O)=O)=CC=C52)=O)=CC=C1)(NC(C)(C)C)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (223.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

=

Concentration Concentration

×

Volume Volume

×

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

×

Volume _(start) Volume _(start)

=

Concentration _(final) Concentration _(final)

×

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. COGAN, et al. SPIRO INDOLINE INHIBITORS OF KIF18A. Patent WO2023028564.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7865 mL	8.9327 mL	17.8654 mL	44.6636 mL
	5 mM	0.3573 mL	1.7865 mL	3.5731 mL	8.9327 mL
	10 mM	0.1787 mL	0.8933 mL	1.7865 mL	4.4664 mL
	15 mM	0.1191 mL	0.5955 mL	1.1910 mL	2.9776 mL
	20 mM	0.0893 mL	0.4466 mL	0.8933 mL	2.2332 mL
	25 mM	0.0715 mL	0.3573 mL	0.7146 mL	1.7865 mL
	30 mM	0.0596 mL	0.2978 mL	0.5955 mL	1.4888 mL
	40 mM	0.0447 mL	0.2233 mL	0.4466 mL	1.1166 mL
	50 mM	0.0357 mL	0.1787 mL	0.3573 mL	0.8933 mL
	60 mM	0.0298 mL	0.1489 mL	0.2978 mL	0.7444 mL
	80 mM	0.0223 mL	0.1117 mL	0.2233 mL	0.5583 mL
	100 mM	0.0179 mL	0.0893 mL	0.1787 mL	0.4466 mL

Keywords

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références