ARD-2128
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MedKoo CAT#: 465419

CAS#: 2222111-87-5

Description: ARD-2128 is a Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer. ARD-2128 achieves 67% oral bioavailability in mice, effectively reduces AR protein and suppresses AR-regulated genes in tumor tissues with oral administration, leading to the effective inhibition of tumor growth in mice without signs of toxicity.

Chemical Structure

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ARD-2128
CAS# 2222111-87-5
Instruction

Theoretical Analysis

MedKoo Cat#: 465419
Name: ARD-2128
CAS#: 2222111-87-5
Chemical Formula: C45H50ClN7O6
Exact Mass: 819.35
Molecular Weight: 820.388
Elemental Analysis: C, 65.88; H, 6.14; Cl, 4.32; N, 11.95; O, 11.70

Price and Availability

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5mg USD 1150 2 Weeks
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Synonym: ARD-2128; ARD2128; ARD 2128;

IUPAC/Chemical Name: N-((1r,3r)-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl)-4-(4-((1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperidin-4-yl)methyl)piperazin-1-yl)benzamide

InChi Key: BWDWHHAZFQBJQL-JABICJEXSA-N

InChi Code: InChI=1S/C45H50ClN7O6/c1-44(2)42(45(3,4)43(44)59-32-11-7-29(25-47)35(46)24-32)49-38(55)28-5-8-30(9-6-28)52-21-19-50(20-22-52)26-27-15-17-51(18-16-27)31-10-12-33-34(23-31)41(58)53(40(33)57)36-13-14-37(54)48-39(36)56/h5-12,23-24,27,36,42-43H,13-22,26H2,1-4H3,(H,49,55)(H,48,54,56)/t36?,42-,43-

SMILES Code: O=C(N[C@H]1C(C)(C)[C@H](OC2=CC=C(C#N)C(Cl)=C2)C1(C)C)C3=CC=C(N4CCN(CC5CCN(C6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)CC5)CC4)C=C3

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 820.39 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: Han X, Zhao L, Xiang W, Qin C, Miao B, McEachern D, Wang Y, Metwally H, Wang L, Matvekas A, Wen B, Sun D, Wang S. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer. J Med Chem. 2021 Aug 25. doi: 10.1021/acs.jmedchem.1c00882. Epub ahead of print. PMID: 34431670.