GM-90257 is a microtubule acetylation inhibitor that binds directly to α-tubulin. GM-90257 prevents the recruitment of α-tubulin acetyltransferase 1 (αTAT1) to the K40 residue in α-tubulin. GM-90257 induces apoptosis in MDA-MB-231 cells and has less effect on MCF-10A or MCF-7 cells with relatively low levels of microtubule acetylation.

Physicochemical Properties

Molecular Formula	C16H14N4OS2
Molecular Weight	342.44
Exact Mass	342.06
CAS #	315703-81-2
PubChem CID	2877425
Appearance	Light brown to brown solid powder
LogP	4.8
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	4
Heavy Atom Count	23
Complexity	408
Defined Atom Stereocenter Count	0
InChi Key	YYYAGFCFCHCRAN-UHFFFAOYSA-N
InChi Code	InChI=1S/C16H14N4OS2/c1-10-14(20-7-8-22-16(20)17-10)13-9-23-15(19-13)18-11-3-5-12(21-2)6-4-11/h3-9H,1-2H3,(H,18,19)
Chemical Name	N-(4-methoxyphenyl)-4-(6-methylimidazo[2,1-b][1,3]thiazol-5-yl)-1,3-thiazol-2-amine
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 Note: This product requires protection from light (avoid light exposure) during transportation and storage.
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

References

[1].Potent Small-Molecule Inhibitors Targeting Acetylated Microtubules as Anticancer Agents Against Triple-Negative Breast Cancer. Biomedicines. 2020 Sep 9;8(9):338.

Solubility Data

Solubility (In Vitro)

DMSO :~12.5 mg/mL (~36.50 mM; with sonication (<60°C))

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.25 mg/mL (3.65 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 12.5 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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: ≥ 1.25 mg/mL (3.65 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 12.5 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD in saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 1.25 mg/mL (3.65 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 12.5 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.9202 mL	14.6011 mL	29.2022 mL
	5 mM	0.5840 mL	2.9202 mL	5.8404 mL
	10 mM	0.2920 mL	1.4601 mL	2.9202 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.