| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
GM-90257 directly targets α-tubulin, a key protein of the microtubule cytoskeleton. It binds to α-tubulin and prevents the recruitment of α-tubulin acetyltransferase 1 (αTAT1) to the K40 residue. This action inhibits the acetylation of microtubules, a post-translational modification that regulates microtubule stability and function.
|
|---|---|
| ln Vitro |
In vitro, GM-90257 selectively induces apoptosis in TNBC cell lines such as MDA-MB-231, with an effective concentration range of 500-1000 nM. It shows significantly less effect on cells with relatively low microtubule acetylation levels, such as MCF-10A or MCF-7 cells. The compound is a valuable tool for studying the role of microtubule acetylation in cancer cell biology, particularly in the context of TNBC and related signaling pathways.
|
| ln Vivo |
In vivo, GM-90257 has been validated in orthotopic TNBC models at a dose of 25 mg/kg. In these models, it has been shown to reduce levels of acetyl-α-tubulin and the proliferation marker Ki67. Further studies are needed to fully elucidate its pharmacokinetic and pharmacodynamic profiles in vivo.
|
| Enzyme Assay |
In vitro binding assays for GM-90257 typically involve assessing its direct binding to α-tubulin. This can be performed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to determine the binding affinity (KD). Competition assays with labeled tubulin or acetylated tubulin antibodies can also be used to evaluate its potency in preventing αTAT1 recruitment to the K40 residue.
|
| Cell Assay |
In vitro cell-based assays for GM-90257 involve treating cancer cell lines, such as MDA-MB-231 (TNBC) and MCF-10A or MCF-7 (control cells with lower acetylation), with varying concentrations of the compound. After treatment, cell viability is assessed using MTT or CellTiter-Glo assays to determine the IC50. Markers of apoptosis (e.g., cleaved PARP, caspase-3) and microtubule acetylation (acetyl-α-tubulin) are evaluated by Western blotting. Cell cycle analysis by flow cytometry can also be performed to assess mitotic arrest.
|
| Animal Protocol |
In vivo efficacy studies are performed using orthotopic TNBC mouse models. GM-90257 is typically administered at a dose of 25 mg/kg. Tumor growth is monitored over time, and at the end of the study, tumors are harvested for immunohistochemical analysis of acetyl-α-tubulin and Ki67 levels. Pharmacodynamic studies may also assess the compound's effect on downstream signaling pathways, such as JNK/AP-1 activation.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of GM-90257 are not extensively characterized in publicly available literature. It is known to have a LogP of 4.8, indicating moderate lipophilicity. The compound is soluble in DMSO at approximately 12.5 mg/mL (~36.50 mM). For in vivo studies, it can be formulated in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline. Further detailed PK studies are needed.
|
| Toxicity/Toxicokinetics |
Toxicological data for GM-90257 are limited as it is a research compound. It has shown a 10-fold selectivity window vs. its analog GM-90631. At its effective concentration in TNBC cells (500-1000 nM), it induces apoptosis while showing less effect on non-TNBC cells. Standard safety precautions should be taken when handling this compound, as with all research chemicals.
|
| References | |
| Additional Infomation |
Additional information: GM-90257 (CAS 315703-81-2) is a research compound available from chemical suppliers. Its molecular formula is C16H14N4OS2 and its molecular weight is 342.44. The compound has a purity of 99% and is primarily used in cancer research, specifically for studying microtubule acetylation in TNBC. It is not approved for clinical use and is strictly for research purposes.
|
| 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
|
| SMILES |
CC1=C(N2C=CSC2=N1)C3=CSC(=N3)NC4=CC=C(C=C4)OC
|
| 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)
|
| 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. View More
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. |
| 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.
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
