WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H207199
CAS#: 2089314-64-5
Description: AOH1996 is a potent PCNA inhibitor. AOH1996, which selectively kills cancer cells. AOH1996 enhances the interaction between PCNA and the largest subunit of RNA polymerase II, RPB1, and dissociates PCNA from actively transcribed chromatin regions, while inducing DNA double-stranded breaks in a transcription-dependent manner. Attenuation of RPB1 interaction with PCNA, by a point mutation in RPB1's PCNA-binding region, confers resistance to AOH1996. Orally administrable and metabolically stable, AOH1996 suppresses tumor growth as a monotherapy or as a combination treatment but causes no discernable side effects.
Hodoodo Cat#: H207199
Name: AOH1996
CAS#: 2089314-64-5
Chemical Formula: C26H22N2O4
Exact Mass: 426.16
Molecular Weight: 426.470
Elemental Analysis: C, 73.23; H, 5.20; N, 6.57; O, 15.01
Synonym: AOH1996; AOH-1996; AOH 1996; NSC789796; NSC 789796; NSC-789796;
IUPAC/Chemical Name: N-[2-[2-(3-methoxyphenoxy)anilino]-2-oxoethyl]naphthalene-1-carboxamide
InChi Key: HDMONPHKMIZXDH-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H22N2O4/c1-31-19-10-7-11-20(16-19)32-24-15-5-4-14-23(24)28-25(29)17-27-26(30)22-13-6-9-18-8-2-3-12-21(18)22/h2-16H,17H2,1H3,(H,27,30)(H,28,29)
SMILES Code: O=C(C1=C2C=CC=CC2=CC=C1)NCC(NC3=CC=CC=C3OC4=CC=CC(OC)=C4)=O
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: Soluble in DMSO
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: Targeting transcription replication conflicts, a major source of endogenous DNA double-stranded breaks and genomic instability could have important anticancer therapeutic implications. Proliferating cell nuclear antigen (PCNA) is critical to DNA replication and repair processes. AOH1996 is an experimental anticancer medication which acts as a small molecule inhibitor of proliferating cell nuclear antigen (PCNA) and as of August 2023 is in Phase I clinical trials for the treatment of solid tumors. It was created to target a specific variant of PCNA found only in cancer cells. This protein is crucial in the body for DNA repair, but targeting it was difficult because of its role in healthy cells. By going after only the variant, it may be possible to selectively target only cancer cells.[5] In vitro testing has suggested that it is effective against a range of cancers including breast, prostate, brain, ovarian, cervical, skin and lung cancers.[6] The substance has been named after the initials and the birth year of Anna Olivia Healey, who died of neuroblastoma in 2006. The funds collected by her parents have helped support the development of the chemical compound. Source: https://en.wikipedia.org/wiki/AOH1996
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The following data is based on the product molecular weight 426.47 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: | |
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In vivo protocol: |
Gu L, Li M, Li CM, Haratipour P, Lingeman R, Jossart J, Gutova M, Flores L, Hyde C, Kenjić N, Li H, Chung V, Li H, Lomenick B, Von Hoff DD, Synold TW, Aboody KS, Liu Y, Horne D, Hickey RJ, Perry JJP, Malkas LH. Small molecule targeting of transcription-replication conflict for selective chemotherapy. Cell Chem Biol. 2023 Jul 26:S2451-9456(23)00221-0. doi: 10.1016/j.chembiol.2023.07.001. Epub ahead of print. PMID: 37531956.