ARD-2051

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 124067

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.

Chemical Structure

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ARD-2051
CAS# 2632305-17-8
Instruction

Theoretical Analysis

MedKoo Cat#: 124067
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

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

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:

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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:

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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.