DB2313

DB2313 is a potent transcription factor PU.1 inhibitor with an apoptosis of 14 nM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects.

Product information

CAS Number: 2170606-74-1

Molecular Weight: 708.83

Formula: C42H41FN8O2

Chemical Name: 2-[4-({2-fluoro-3-[(4-{6-[N'-(propan-2-yl)carbamimidoyl]-1H-1,3-benzodiazol-2-yl}phenoxy)methyl]phenyl}methoxy)phenyl]-N'-(propan-2-yl)-1H-1,3-benzodiazole-6-carboximidamide

Smiles: CC(C)N=C(N)C1C=C2NC(=NC2=CC=1)C1C=CC(=CC=1)OCC1C=CC=C(COC2C=CC(=CC=2)C2NC3C=C(C=CC=3N=2)C(N)=NC(C)C)C=1F

InChiKey: NUVPJXUYFGWDGB-UHFFFAOYSA-N

InChi: InChI=1S/C42H41FN8O2/c1-24(2)46-39(44)28-12-18-34-36(20-28)50-41(48-34)26-8-14-32(15-9-26)52-22-30-6-5-7-31(38(30)43)23-53-33-16-10-27(11-17-33)42-49-35-19-13-29(21-37(35)51-42)40(45)47-25(3)4/h5-21,24-25H,22-23H2,1-4H3,(H2,44,46)(H2,45,47)(H,48,50)(H,49,51)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

How to use

In Vitro:

DB2313 treatment leads to a profound decrease in the growth of PU.1 URE–/– acute myeloid leukemia (AML) cells (IC50 of 7.1 μM), while showing little effect on normal hematopoietic cells at similar concentrations. DB2313 treatment leads to a 3.5-fold increase in apoptotic cells in murine PU.1 URE–/– AML cells. DB2313 also leads to a significant decrease in clonogenicity in the second and third rounds of plating and a complete disruption of clonogenic capacity in the fourth and higher rounds of plating. In AML cells, DB2313 decreases PU.1 occupancy on E2f1, Junb, and Csf1r promoters.

In Vivo:

DB2313 (17 mg/kg; i.p.; three times per week; for 3 weeks) treatment decreases leukemia progression and results in increased survival in mice.

Products are for research use only. Not for human use.