MedKoo Cat#: 408055 | Name: ARD-266

Description:

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

ARD-266 is a potent PROTAC Degrader (DC50 = 0.2 ~1 nM, IC50 = 1~6 nM). ARD-266 effectively induces degradation of AR protein in AR-positive (AR+) LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2−1 nM. ARD-266 is capable of reducing the AR protein level by >95% in these AR+ prostate cancer cell lines and effectively reduces ARregulated gene expression suppression.

Chemical Structure

ARD-266
CAS#2666951-70-6

Theoretical Analysis

MedKoo Cat#: 408055

Name: ARD-266

CAS#: 2666951-70-6

Chemical Formula: C52H59ClN6O7

Exact Mass: 914.4134

Molecular Weight: 915.53

Elemental Analysis: C, 68.22; H, 6.50; Cl, 3.87; N, 9.18; O, 12.23

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
ARD-266; ARD 266; ARD266; PROTAC Degrader
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)piperidin-1-yl)-3-oxo-1-phenylpropyl)-4-hydroxy-1-((R)-3-methyl-2-(3-methylisoxazol-5-yl)butanoyl)pyrrolidine-2-carboxamide
InChi Key
RTNONCBKGZNCJS-LJLQSONVSA-N
InChi Code
InChI=1S/C52H59ClN6O7/c1-31(2)45(43-25-32(3)57-66-43)48(64)59-30-38(60)26-42(59)47(63)55-41(35-11-9-8-10-12-35)28-44(61)58-23-21-34(22-24-58)14-13-33-15-17-36(18-16-33)46(62)56-49-51(4,5)50(52(49,6)7)65-39-20-19-37(29-54)40(53)27-39/h8-12,15-20,25,27,31,34,38,41-42,45,49-50,60H,21-24,26,28,30H2,1-7H3,(H,55,63)(H,56,62)/t38-,41+,42+,45-,49-,50-/m1/s1
SMILES Code
O=C([C@H]1N(C([C@@H](C2=CC(C)=NO2)C(C)C)=O)C[C@H](O)C1)N[C@H](C3=CC=CC=C3)CC(N4CCC(C#CC5=CC=C(C(N[C@H]6C(C)(C)[C@H](OC7=CC=C(C#N)C(Cl)=C7)C6(C)C)=O)C=C5)CC4)=O
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
Soluble in DMSO
Shelf Life
>3 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
More Info
Androgen receptor (AR) is a validated therapeutic target for the treatment of metastatic castration-resistant prostate cancer (mCRPC).

Preparing Stock Solutions

The following data is based on the product molecular weight 915.53 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
Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands Xin HanLijie ZhaoWeiguo XiangChong QinBukeyan MiaoTianfeng XuMi WangChao-Yie YangKrishnapriya ChinnaswamyJeanne StuckeyShaomeng Wang* Journal of Medicinal Chemistry, Articles ASAP (Article)Subscribed Access Publication Date (Web):December 5, 2019