WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H124067
CAS#: 2632305-17-8
Description: ARD-2051 is a potent and orally efficacious androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM and Dmax >90% in inducing AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines, potently and effectively suppresses AR-regulated genes, and inhibits cancer cell growth. ARD-2051 achieves a good oral bioavailability and pharmacokinetic profile in mouse, rat, and dog. A single oral dose of ARD-2051 strongly reduces AR protein and suppresses AR-regulated gene expression in the VCaP xenograft tumor tissue in mice. Oral administration of ARD-2051 effectively inhibits VCaP tumor growth and causes no signs of toxicity in mice. ARD-2051 is a promising AR degrader for advanced preclinical development for the treatment of AR+ human cancers.
Hodoodo Cat#: H124067
Name: ARD-2051
CAS#: 2632305-17-8
Chemical Formula: C43H45ClN8O5
Exact Mass: 788.32
Molecular Weight: 789.330
Elemental Analysis: C, 65.43; H, 5.75; Cl, 4.49; N, 14.20; O, 10.13
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Synonym: ARD-2051; ARD 2051; ARD2051
IUPAC/Chemical Name: 2-chloro-4-((3S)-8-(4-(4-(1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)azetidin-3-yl)piperazine-1-carbonyl)phenyl)-3-methyl-2,8-diazaspiro[4.5]decan-2-yl)benzonitrile
InChi Key: WBMJNGGUHCHFHY-YTCZSSRZSA-N
InChi Code: InChI=1S/C43H45ClN8O5/c1-27-22-43(26-51(27)32-7-4-29(23-45)36(44)21-32)12-14-47(15-13-43)30-5-2-28(3-6-30)40(55)49-18-16-48(17-19-49)33-24-50(25-33)31-8-9-34-35(20-31)42(57)52(41(34)56)37-10-11-38(53)46-39(37)54/h2-9,20-21,27,33,37H,10-19,22,24-26H2,1H3,(H,46,53,54)/t27-,37?/m0/s1
SMILES Code: ClC1=C(C#N)C=CC(N2CC3(CCN(C4=CC=C(C(N5CCN(C6CN(C7=CC(C(N(C8C(NC(CC8)=O)=O)C9=O)=O)=C9C=C7)C6)CC5)=O)C=C4)CC3)C[C@@H]2C)=C1
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 789.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
Han X, Zhao L, Xiang W, Miao B, Qin C, Wang M, Xu T, McEachern D, Lu J, Wang Y, Metwally H, Yang CY, Kirchhoff PD, Wang L, Matvekas A, Takyi-Williams J, Wen B, Sun D, Ator M, Mckean R, Wang S. Discovery of ARD-2051 as a Potent and Orally Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer. J Med Chem. 2023 Jun 29. doi: 10.1021/acs.jmedchem.3c00405. Epub ahead of print. PMID: 37382562.