1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin Kinesin
  3. AM-5308

AM-5308 is the inhibitor for KIF18A (IC50=47 nM) that inhibits KIF18A-mediated microtubule ATPase activity. AM-5308 activates mitotic checkpoints, regulates cell division processes, including chromosome segregation and spindle assembly. AM-5308 exhibits antitumor activity.

For research use only. We do not sell to patients.

AM-5308 Chemical Structure

AM-5308 Chemical Structure

CAS No. : 2410796-89-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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Description

AM-5308 is the inhibitor for KIF18A (IC50=47 nM) that inhibits KIF18A-mediated microtubule ATPase activity. AM-5308 activates mitotic checkpoints, regulates cell division processes, including chromosome segregation and spindle assembly. AM-5308 exhibits antitumor activity[1][2].

IC50 & Target

IC50: 0.047 µM (KIF18A motor); 0.224 µM (KIF19A motor); 17.73 µM (KIF18B motor)[2]

In Vitro

AM-5308 (0-10 μM, 24 h) exhibits cytotoxicity in human bone marrow cell, arrests the cell cycle of MDA-MB-157 and human bone marrow cell in mitosis phase (EC50 for MDA-MB-157 is 0.041 μM)[2].

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

Cell Cycle Analysis[2]

Cell Line: human bone marrow cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Arrested the cell cycle at mitosis phase.
In Vivo

AM-5308 (25 mg/kg, ip, once daily for 2 days) exhibits antitumor activity in mouse OVCAR-3 xenograft models[2].

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

Animal Model: mouse OVCAR-3 xenograft models[2]
Dosage: 25 mg/kg
Administration: ip, once daily for 2 days
Result: Inhibited the tumor growth.
Molecular Weight

529.65

Formula

C26H35N5O5S

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

C[C@@H](OCC1)CN1C2=NC(NC(C3=C(C=C(C=C3)NS(CCO)(=O)=O)N4CCC5(CC4)CC5)=O)=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (94.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8880 mL 9.4402 mL 18.8804 mL
5 mM 0.3776 mL 1.8880 mL 3.7761 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

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In Vivo:

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

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% (20% SBE-β-CD in Saline)

    Solubility: 2 mg/mL (3.78 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.15%

References

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 1.8880 mL 9.4402 mL 18.8804 mL 47.2010 mL
5 mM 0.3776 mL 1.8880 mL 3.7761 mL 9.4402 mL
10 mM 0.1888 mL 0.9440 mL 1.8880 mL 4.7201 mL
15 mM 0.1259 mL 0.6293 mL 1.2587 mL 3.1467 mL
20 mM 0.0944 mL 0.4720 mL 0.9440 mL 2.3600 mL
25 mM 0.0755 mL 0.3776 mL 0.7552 mL 1.8880 mL
30 mM 0.0629 mL 0.3147 mL 0.6293 mL 1.5734 mL
40 mM 0.0472 mL 0.2360 mL 0.4720 mL 1.1800 mL
50 mM 0.0378 mL 0.1888 mL 0.3776 mL 0.9440 mL
60 mM 0.0315 mL 0.1573 mL 0.3147 mL 0.7867 mL
80 mM 0.0236 mL 0.1180 mL 0.2360 mL 0.5900 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AM-5308
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