1297538-32-9 Usage
Description
ODM-201 is a novel androgen receptor (AR) antagonist designed to inhibit the growth of prostate cancer cells. It works by binding to the AR and inhibiting testosterone-induced AR nuclear translocation, making it a promising next-generation therapy for prostate cancer. ODM-201 is particularly effective in patients with progressive metastatic castration-resistant prostate cancer and can overcome resistance issues that arise during AR-targeted therapies.
Uses
Used in Prostate Cancer Treatment:
ODM-201 is used as a next-generation androgen receptor-directed therapy for prostate cancer. It is effective in inhibiting the activity of some mutant ARs emerging during antiandrogen therapies, including the F876L mutation version which is resistant to enzalutamide and ARN-509 (the second-generation antiandrogens). This makes ODM-201 a potential treatment option for patients with progressive metastatic castration-resistant prostate cancer.
Used in Anticancer Applications:
ODM-201 is used as an anticancer agent in the treatment of prostate cancer. It inhibits AR transactivation in U2OS osteosarcoma cells expressing human wild-type and mutant ARs. ODM-201 also prevents androgen-induced AR nuclear translocation in AR-overexpressing HS-HEK293 and LNCaP cells and suppresses androgen-induced proliferation of VCaP cells.
Used in Preclinical Models:
ODM-201 is used in in vivo studies to evaluate its efficacy in reducing tumor growth. In a VCaP castrated mouse xenograft model, ODM-201 (50 mg/kg per day) has been shown to reduce tumor growth. Additionally, it inhibits tumor growth without increasing serum testosterone levels in a VCaP intact mouse xenograft model, demonstrating its potential as a therapeutic agent for prostate cancer treatment.
References
Moilanen, Anu Maarit, et al. "Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies." Sci Rep 5.2(2015):12007.
Fizazi, Karim, et al. "ODM-201, a new generation androgen receptor inhibitor for castration-resistant prostate cancer: Preclinical and phase I data." Genitourinary Cancers Symposium of the Conquer-Cancer-Foundation of 2013.
Fizazi, K, et al. "Activity and safety of ODM-201 in patients with progressive metastatic castration-resistant prostate cancer (ARADES): an open-label phase 1 dose-escalation and randomised phase 2 dose expansion trial." Lancet Oncology 5.9(2014):975-85.
Check Digit Verification of cas no
The CAS Registry Mumber 1297538-32-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,9,7,5,3 and 8 respectively; the second part has 2 digits, 3 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1297538-32:
(9*1)+(8*2)+(7*9)+(6*7)+(5*5)+(4*3)+(3*8)+(2*3)+(1*2)=199
199 % 10 = 9
So 1297538-32-9 is a valid CAS Registry Number.
1297538-32-9Relevant articles and documents
Pyrazoleamide derivative and synthesis method and application
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, (2022/01/10)
The present invention discloses a pyrazoleamide derivative and a synthetic method and application as an androgen receptor antagonist and the preparation of anti-prostate cancer drugs. The present invention provides a method of synthesizing a pentabasole r
Method for preparing antitumor drug darolutamide
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Paragraph 0059-0065, (2020/05/30)
The invention relates to a method for preparing an antitumor drug darolutamide. A one-step Suzuki reaction is carried out, and then deprotection, hydroxylamine condensation and amide condensation reactions are carried out to obtain the darolutamide. The method has the advantages of few reaction steps, high reaction yield of each step, and simplicity in operation, so the total yield of the whole route is high, and the method has good experiment operationality.
Preparation method of N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazol-3-carboxamide
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, (2020/01/03)
The invention relates to a preparation method of N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazol-3-carboxamide, and in particular relates to two novel methods for preparing an intermediate (S)-4-(1-(2-aminopropyl)-1H-pyrazol-3-yl)-2-chlorobenzonitrile and a method for preparing N-[(1S)-2-[3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl]-1-methylethyl]-5-(1-hydroxyethyl)-1H-pyrazol-3-carboxamide from the intermediate.