ARD-2128|CAS 2222111-87-5|DC Chemicals

Cas No.:	2222111-87-5
Chemical Name:	N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]piperidin-4-yl]methyl]piperazin-1-yl]benzamide
Synonyms:	N-[3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxopiperidin-3-yl)-
SMILES:	ClC1=C(C#N)C([H])=C([H])C(=C1[H])OC1([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])(C1(C([H])([H])[H])C([H])([H])[H])N([H])C(C1C([H])=C([H])C(=C([H])C=1[H])N1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C([H])([H])C1([H])C([H])([H])C([H])([H])N(C2C([H])=C([H])C3C(N(C4([H])C(N([H])C(C([H])([H])C4([H])[H])=O)=O)C(C=3C=2[H])=O)=O)C([H])([H])C1([H])[H])=O
Formula:	C₄₅H₅₀ClN₇O₆
M.Wt:	820.3748
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Han X, et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;10.1021/acs.jmedchem.1c00882.

Target:	IC50: 4 nM (VCaP), 5 μM (LNCaP)[1]
In Vivo:	ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours[1]. ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice[1]. ARD-2128 (5mg/kg; p.o.) treatment shows the Cmax, AUC0-t and t1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively[1]. Animal Model: SCID mice[1] Dosage: 20 mg/kg Administration: Oral Result: Reducing the level of AR protein in mice after 24 hours. Animal Model: SCID mice[1] Dosage: 10, 20, and 40 mg/kg Administration: P.o.; daily for 21 days Result: Inhibits tumor growth by 46, 69, and 63%, respectively. Animal Model: Male ICR Mice[1] Dosage: 5 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: The Cmax, AUC0-t and t1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.
In Vitro:	ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC50 values of 4 nM and 5 nM, respectively[1]. ARD-2128 (1, 10, 100, and 1000 nM; 24 hours) effectively reduces the AR protein level by >50% at 1 nM and achieves the AR degradation of >90% at 10, 100, and 1000 nM, respectively, in VCaP cell[1]. Cell Viability Assay[1] Cell Line: VCaP cell Concentration: 1, 10, 100, and 1000 nM Incubation Time: 24 hours Result: Reduces the AR protein level and achieves the AR degradation.
References:	[1]. Han X, et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;10.1021/acs.jmedchem.1c00882.

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