WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H124845
CAS#: N/A
Description: ARD-1676 is a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer. ARD-1676 has DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, respectively, and IC50 values of 11.5 and 2.8 nM in VCaP and LNCaP cell lines, respectively. ARD-1676 effectively induces degradation of a broad panel of clinically relevant AR mutants. ARD-1676 has an oral bioavailability of 67, 44, 31, and 99% in mice, rats, dogs, and monkeys, respectively. Oral administration of ARD-1676 effectively reduces the level of AR protein in the VCaP tumor tissue in mice and inhibits tumor growth in the VCaP mouse xenograft tumor model without any sign of toxicity.
Hodoodo Cat#: H124845
Name: ARD-1676
CAS#: N/A
Chemical Formula: C44H46ClN7O5
Exact Mass: 787.32
Molecular Weight: 788.350
Elemental Analysis: C, 67.04; H, 5.88; Cl, 4.50; N, 12.44; O, 10.15
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Synonym: ARD-1676; ARD1676; ARD 1676
IUPAC/Chemical Name: 2-chloro-4-((3S)-8-(4-(4-((6-(2,6-dioxopiperidin-3-yl)-5,7-dioxo-3,5,6,7-tetrahydropyrrolo[3,4-f]isoindol-2(1H)-yl)methyl)piperidine-1-carbonyl)phenyl)-3-methyl-2,8-diazaspiro[4.5]decan-2-yl)benzonitrile
InChi Key: GAXWAKXJBZHVQF-ZVENJKCTSA-N
InChi Code: InChI=1S/C44H46ClN7O5/c1-27-21-44(26-51(27)34-7-4-30(22-46)37(45)20-34)12-16-49(17-13-44)33-5-2-29(3-6-33)41(55)50-14-10-28(11-15-50)23-48-24-31-18-35-36(19-32(31)25-48)43(57)52(42(35)56)38-8-9-39(53)47-40(38)54/h2-7,18-20,27-28,38H,8-17,21,23-26H2,1H3,(H,47,53,54)/t27-,38?/m0/s1
SMILES Code: ClC1=CC(N2CC3(CCN(C4=CC=C(C(N5CCC(CN6CC(C=C(C(N(C7C(NC(CC7)=O)=O)C8=O)=O)C8=C9)=C9C6)CC5)=O)C=C4)CC3)C[C@@H]2C)=CC=C1C#N
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: | |
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The following data is based on the product molecular weight 788.35 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.
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: |