ARD-2128
CAS No. 2222111-87-5
ARD-2128 ( —— )
Catalog No. M28233 CAS No. 2222111-87-5
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
2MG | 308 | Get Quote |
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5MG | 520 | Get Quote |
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10MG | 750 | Get Quote |
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25MG | 1143 | Get Quote |
|
50MG | 1521 | Get Quote |
|
100MG | 2061 | Get Quote |
|
200MG | Get Quote | Get Quote |
|
500MG | Get Quote | Get Quote |
|
1G | Get Quote | Get Quote |
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Biological Information
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Product NameARD-2128
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NoteResearch use only, not for human use.
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Brief DescriptionARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity.
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DescriptionARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.(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 IC 50 values of 4 nM and 5 nM, respectively . 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 . Cell Viability Assay 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.(In Vivo):ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours . ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice . ARD-2128 (5mg/kg; p.o.) treatment shows the C max , AUC 0-t and t 1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively . Animal Model: SCID mice Dosage: 20 mg/kg Administration: Oral Result: Reducing the level of AR protein in mice after 24 hours. Animal Model: SCID mice 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 Dosage: 5 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: The C max , AUC 0-t and t 1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.
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Synonyms——
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PathwayEndocrinology/Hormones
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TargetAndrogen Receptor (AR)
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RecptorTNIK
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Research Area——
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Indication——
Chemical Information
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CAS Number2222111-87-5
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Formula Weight820.4
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Molecular FormulaC45H50ClN7O6
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Purity>98% (HPLC)
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Solubility——
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SMILESCC(C)([C@H](C1(C)C)NC(c(cc2)ccc2N2CCN(CC(CC3)CCN3c(cc3)cc(C(N4C(CCC(N5)=O)C5=O)=O)c3C4=O)CC2)=O)[C@H]1Oc(cc1)cc(Cl)c1C#N
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Shengyong Yang, Linli Li. Preparation of TNIK inhibitor compounds as antitumor agents. CN113773316A
molnova catalog
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