ARD-61
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 465420

CAS#: 2316837-08-6

Description: ARD-61 is an AR antagonist and PROTAC AR degrader.

Chemical Structure

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ARD-61
CAS# 2316837-08-6
Instruction

Theoretical Analysis

MedKoo Cat#: 465420
Name: ARD-61
CAS#: 2316837-08-6
Chemical Formula: C61H71ClN8O7S
Exact Mass: 1,094.49
Molecular Weight: 1,095.798
Elemental Analysis: C, 66.86; H, 6.53; Cl, 3.24; N, 10.23; O, 10.22; S, 2.93

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5mg USD 2650 2 Weeks
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Synonym: ARD-61; ARD61; ARD 61;

IUPAC/Chemical Name: (2S,4R)-N-((S)-3-(4-((4-(((1r,3r)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl)carbamoyl)phenyl)ethynyl)-[1,4'-bipiperidin]-1'-yl)-1-(4-(4-methylthiazol-5-yl)phenyl)-3-oxopropyl)-4-hydroxy-1-((R)-3-methyl-2-(3-methylisoxazol-5-yl)butanoyl)pyrrolidine-2-carboxamide

InChi Key: RGPUSLXMPBTXNU-MLMZQBPXSA-N

InChi Code: InChI=1S/C61H71ClN8O7S/c1-36(2)53(51-29-37(3)67-77-51)57(75)70-34-46(71)30-50(70)56(74)65-49(41-15-17-42(18-16-41)54-38(4)64-35-78-54)32-52(72)69-27-23-45(24-28-69)68-25-21-40(22-26-68)10-9-39-11-13-43(14-12-39)55(73)66-58-60(5,6)59(61(58,7)8)76-47-20-19-44(33-63)48(62)31-47/h11-20,29,31,35-36,40,45-46,49-50,53,58-59,71H,21-28,30,32,34H2,1-8H3,(H,65,74)(H,66,73)/t46-,49+,50+,53-,58-,59-/m1/s1

SMILES Code: ClC1=CC(O[C@H]2C(C)(C)[C@H](NC(C3=CC=C(C#CC4CCN(C5CCN(C(C[C@@H](C6=CC=C(C7=C(C)N=CS7)C=C6)NC([C@H]8N(C([C@@H](C9=CC(C)=NO9)C(C)C)=O)C[C@H](O)C8)=O)=O)CC5)CC4)C=C3)=O)C2(C)C)=CC=C1C#N

Appearance: Solid powder

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 1,095.80 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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1: Zhao L, Han X, Lu J, McEachern D, Wang S. A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro and tumor growth in vivo. Neoplasia. 2020 Oct;22(10):522-532. doi: 10.1016/j.neo.2020.07.002. PMID: 32928363; PMCID: PMC7498667.

2: Kregel S, Wang C, Han X, Xiao L, Fernandez-Salas E, Bawa P, McCollum BL, Wilder-Romans K, Apel IJ, Cao X, Speers C, Wang S, Chinnaiyan AM. Androgen receptor degraders overcome common resistance mechanisms developed during prostate cancer treatment. Neoplasia. 2020 Feb;22(2):111-119. doi: 10.1016/j.neo.2019.12.003. Epub 2020 Jan 10. PMID: 31931431; PMCID: PMC6957805.