PeptideDB

ST-401 2419942-78-0

ST-401 2419942-78-0

CAS No.: 2419942-78-0

ST-401 is a microtubule targeting agent (MTA) and a brain-permeable microtubule (MT) assembly inhibitor. ST-401 disrupts
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This product is for research use only, not for human use. We do not sell to patients.

ST-401 is a microtubule targeting agent (MTA) and a brain-permeable microtubule (MT) assembly inhibitor. ST-401 disrupts microtubule (MT) function by mildly and reversibly reducing MT assembly, thereby inducing mitotic delay and interphase cell death. ST-401 exhibits potent anti-tumor activity.

Physicochemical Properties


Molecular Formula C24H20N2O
Molecular Weight 352.43
CAS # 2419942-78-0
Appearance White to light yellow solid powder
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)

Biological Activity


ln Vitro ST-401 is a hybrid molecule that combines a secondary alcohol and a quinoline in one structure. ST-401 competes for 89% of the binding of [3H]colchicine to tubulin. In a turbidity assay, ST-401 inhibits tubulin assembly with an IC50 of 1.1 µM. In a precipitation assay that measures the release of free tubulin, ST-401 inhibits tubulin assembly with an IC50 of 3.2 µM[1]. ST-401 exhibits similar low nanomolar antitumor activity in most human cancer cell lines, including six glioma lines (SF-268, SF-295, SF-539, SNB-19, SNB-75, and U251: IC50 of 23-69 nM)[1]. ST-401 exhibits low nanomolar antitumor activity in PD-glioma (IC50: 24-47 nM)[1]. ST-401 (72 hours) reduced overall cell viability in MGG8 and T98G cells with comparable IC50 values (14 and 36 nM, respectively) [1].
ln Vivo ST-401 (20 mg/kg; intraperitoneal injection; twice daily; 5 days a week for 4 weeks) showed significant antitumor activity without excessive toxicity in a xenograft flank tumor mouse model [1 ].
Animal Protocol Animal/Disease Models:Nude mice (10-14 weeks of age) injection with COLO205 cells[1]
Doses: 20 mg/kg
Route of Administration: i.p; bidaily; 5 days/week for 4 weeks
Experimental Results: Resulted in significant antitumor activity.
References

[1]. A brain-penetrant microtubule-targeting agent that disrupts hallmarks of glioma tumorigenesis. Neurooncol Adv. 2020 Dec 3;3(1):vdaa165.


Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8374 mL 14.1872 mL 28.3744 mL
5 mM 0.5675 mL 2.8374 mL 5.6749 mL
10 mM 0.2837 mL 1.4187 mL 2.8374 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.