Keywords

• Galeterone
• TOK-001
• best price

Quick Details

• ProName: Galeterone
• CasNo: 851983-85-2
• Molecular Formula: C26H32N2O
• Application: For laboratory use only- not intended ...
• ProductionCapacity: 1 Kilogram/Month
• Purity: ≥98%
• Storage: room temperature
• Transportation: by air
• LimitNum: 1 Gram

Superiority

We are a CRO company, and our Research and Development team is consisted of PhDs and Masters in chemistry and pharmacy.

We are committed to protect our customer’s privacy with the highest level of ethical standard. Our dedicated team will follow up on every order and provide instant feedback on the status to our customer.

We stand behind our product by providing a complete QA report. The test data of customer order can be provided upon request.

We make our efforts to offer customer innovative, customized, high-quality service.

Our custom manufacturing encompasses everything from pharmaceutical intermediates to API.

Details

TOK-001 is a multifunctional antiandrogen and CYP17 inhibitor (IC₅₀=47 nM) in castration resistant prostate cancer (CRPC). IC50 & Target: IC50: 47 nM (CYP17). In Vitro: TOK-001 affords strong CYP17 lyase inhibition, with IC₅₀ of 47 nM. TOK-001 is both a CYP17A1 inhibitor and androgen receptor antagonist and the similarity of these binding modes is likely the reason for this dual mechanism of action.This CYP17A1 binds abiraterone and TOK-001 with absorbance decreases at 402 nm and increases at 424 nm, consistent with nitrogen binding to the heme iron (type II interaction) with K_d of <100 nM. When LNCaP cells are cultured in medium supplemented with charcoal-stripped serum (CSS, T<1 nM) followed by treatment with increasing concentrations of TOK-001, the steady-state levels of AR protein are markedly decreased (up to 84%, 15 μM TOK-001). In LAPC-4 cells, abiraterone alcohol reduced AR expression to a greater extent than TOK-001 at concentrations greater than or equal to 1 μM. When LNCaP cells are treated with 20 μM TOK-001 for 24 h, AR mRNA levels are reduced by 38%. In Vivo: Mice inoculated with LAPC-4 tumors are treated subcutaneously with 0.15 mmol/kg of TOK-001 twice daily. Mice treated with TOK-001 have smaller average tumor volume on day 31 when compared to control (p= 0.0001). TOK-001 treatment also significantly reduces the growth rate of tumor growth compared to control (p<0.0001). Upon excision, final tumor weights are also significantly reduced in animals treated with TOK-001 compared to animals treated with control, and castration (p<0.05)^[