ASP9521
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MedKoo CAT#: 205818

CAS#: 1126084-37-4

Description: ASP9521 is a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3). 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.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 65 Same Day
25mg USD 150 Same Day
50mg USD 250 Same Day
100mg USD 450 Same Day
200mg USD 850 Same Day
500mg USD 1750 Same Day
1g USD 2750 2 Weeks
2g USD 4750 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-08-14. Prices are subject to change without notice.

ASP9521, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205818
Name: ASP9521
CAS#: 1126084-37-4
Chemical Formula: C19H26N2O3
Exact Mass: 330.19434
Molecular Weight: 330.42
Elemental Analysis: C, 69.06; H, 7.93; N, 8.48; O, 14.53


Synonym: ASP9521; ASP-9521; ASP 9521. AKR1C3 inhibitor ; 17HSD5 inhibitor

IUPAC/Chemical Name: (4-(2-hydroxy-2-methylpropyl)piperidin-1-yl)(5-methoxy-1H-indol-2-yl)methanone.

InChi Key: OXSCPDKUZWPWFR-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: O=C(N1CCC(CC(C)(O)C)CC1)C(N2)=CC3=C2C=CC(OC)=C3


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

  
 
 
 


References

1: Kikuchi A, Furutani T, Azami H, Watanabe K, Niimi T, Kamiyama Y, Kuromitsu S,  Baskin-Bey E, Heeringa M, Ouatas T, Enjo K. In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3). Invest New Drugs. 2014 Jul 1. [Epub ahead of print] PubMed PMID: 24981575.

2: Loriot Y, Fizazi K, Jones RJ, Van den Brande J, Molife RL, Omlin A, James ND, Baskin-Bey E, Heeringa M, Baron B, Holtkamp GM, Ouatas T, De Bono JS. Safety, tolerability and anti-tumour activity of the androgen biosynthesis inhibitor ASP9521 in patients with metastatic castration-resistant prostate cancer: multi-centre phase I/II study. Invest New Drugs. 2014 Apr 27. [Epub ahead of print] PubMed PMID: 24771350.