Description
AI-10-49 is an inhibitor that binds the transcription factor fusion CBFβ-SMMHC. AI-10-49, that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1. AI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics, and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death. These data suggest that direct inhibition of the oncogenic CBFβ-SMMHC fusion protein may be an effective therapeutic approach for inv(16) AML, and they provide support for transcription factor targeted therapy in other cancers.
Product information
CAS Number: 1256094-72-0
Molecular Weight: 660.52
Formula: C30H22F6N6O5
Synonym:
AI 10 49
AI-10-49
AI 10-49
AI10-49
AI-1049
AI 1049
AI1049
Chemical Name: 2,2'-(((oxybis(ethane-2,1-diyl))bis(oxy))bis(pyridine-5,2-diyl))bis(5-(trifluoromethoxy)-1H-benzo[d]imidazole)
Smiles: FC(F)(F)OC1=CC=C2NC(=NC2=C1)C1=CC=C(C=N1)OCCOCCOC1=CN=C(C=C1)C1NC2=CC=C(C=C2N=1)OC(F)(F)F
InChiKey: WJBSSBFGPKTMQQ-UHFFFAOYSA-N
InChi: InChI=1S/C30H22F6N6O5/c31-29(32,33)46-17-1-5-21-25(13-17)41-27(39-21)23-7-3-19(15-37-23)44-11-9-43-10-12-45-20-4-8-24(38-16-20)28-40-22-6-2-18(14-26(22)42-28)47-30(34,35)36/h1-8,13-16H,9-12H2,(H,39,41)(H,40,42)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
References:
- Castilla LH, Bushweller JH. Molecular Basis and Targeted Inhibition of CBFβ-SMMHC Acute Myeloid Leukemia. Adv Exp Med Biol. 2017;962:229-244. doi: 10.1007/978-981-10-3233-2_15. Review. PubMed PMID: 28299661.
- Illendula A, Pulikkan JA, Zong H, Grembecka J, Xue L, Sen S, Zhou Y, Boulton A, Kuntimaddi A, Gao Y, Rajewski RA, Guzman ML, Castilla LH, Bushweller JH. Chemical biology. A small-molecule inhibitor of the aberrant transcription factor CBFβ-SMMHC delays leukemia in mice. Science. 2015 Feb 13;347(6223):779-84. doi: 10.1126/science.aaa0314. PubMed PMID: 25678665; PubMed Central PMCID: PMC4423805.
Products are for research use only. Not for human use.
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