Details
Stereochemistry | ACHIRAL |
Molecular Formula | C19H26N2O3 |
Molecular Weight | 330.4213 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C2NC(=CC2=C1)C(=O)N3CCC(CC(C)(C)O)CC3
InChI
InChIKey=OXSCPDKUZWPWFR-UHFFFAOYSA-N
InChI=1S/C19H26N2O3/c1-19(2,23)12-13-6-8-21(9-7-13)18(22)17-11-14-10-15(24-3)4-5-16(14)20-17/h4-5,10-11,13,20,23H,6-9,12H2,1-3H3
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P42330|||Q9UII3 Gene ID: 8644.0 Gene Symbol: AKR1C3 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/24981575 |
11.0 nM [IC50] |
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300000042376
Created by
admin on Sat Dec 16 18:55:26 GMT 2023 , Edited by admin on Sat Dec 16 18:55:26 GMT 2023
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25210792
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admin on Sat Dec 16 18:55:26 GMT 2023 , Edited by admin on Sat Dec 16 18:55:26 GMT 2023
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AA79G37CPR
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admin on Sat Dec 16 18:55:26 GMT 2023 , Edited by admin on Sat Dec 16 18:55:26 GMT 2023
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ASP-9521
Created by
admin on Sat Dec 16 18:55:26 GMT 2023 , Edited by admin on Sat Dec 16 18:55:26 GMT 2023
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PRIMARY | MedKoo CAT NO: 205818; CAS NO: 1126084-37-4; Description: ASP9521 is a novel, selective, orally bioavailable inhibitor of 17.BETA.-hydroxysteroid dehydrogenase type 5 (17.BETA.HSD5AKR1C3). ASP9521 has demonstrated anti-tumour activity in in vitro and in vivo preclinical models. ASP9521 inhibited conversion of androstenedione (AD) into testosterone (T) by recombinant human or cynomolgus monkey AKR1C3 in a concentration-dependent manner (IC50,human: 11 nmol/L - IC50,monkey: 49 nmol/L). ASP9521 showed >100-fold selectivity for AKR1C3 over the isoform AKR1C2. In LNCaP-AKR1C3 cells, ASP9521 suppressed AD-dependent PSA production and cell proliferation. In patients with mCRPC, ASP9521 demonstrated dose-proportional increase in exposure over the doses evaluated, with an acceptable safety and tolerability profile. However, the novel androgen biosynthesis inhibitor showed no relevant evidence of clinical activity. (Last update: 11/18/2015). | ||
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C133224
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admin on Sat Dec 16 18:55:26 GMT 2023 , Edited by admin on Sat Dec 16 18:55:26 GMT 2023
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1126084-37-4
Created by
admin on Sat Dec 16 18:55:26 GMT 2023 , Edited by admin on Sat Dec 16 18:55:26 GMT 2023
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PRIMARY |
ACTIVE MOIETY