WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407211
Description: AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells. AZ6102 can be formulated well in a clinically relevant intravenous solution at 20 mg/mL, has demonstrated good pharmacokinetics in preclinical species, and shows low Caco2 efflux to avoid possible tumor resistance mechanisms. The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ß-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is known to inhibit the Wnt pathway via increased stabilization of Axin.
MedKoo Cat#: 407211
Chemical Formula: C25H28N6O
Exact Mass: 428.23246
Molecular Weight: 428.54
Elemental Analysis: C, 70.07; H, 6.59; N, 19.61; O, 3.73
AZ6102, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Synonym: AZ6102; AZ-6102; AZ 6102.
IUPAC/Chemical Name: 2-(4-(6-((3R,5S)-3,5-dimethylpiperazin-1-yl)-4-methylpyridin-3-yl)phenyl)-7-methyl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one
InChi Key: WCPTUQOMNJBIET-CALCHBBNSA-N
InChi Code: InChI=1S/C25H28N6O/c1-15-11-22(31-13-16(2)27-17(3)14-31)26-12-21(15)18-5-7-19(8-6-18)23-28-24-20(25(32)29-23)9-10-30(24)4/h5-12,16-17,27H,13-14H2,1-4H3,(H,28,29,32)/t16-,17+
SMILES Code: O=C1C2=C(N(C)C=C2)N=C(C3=CC=C(C4=C(C)C=C(N5C[C@@H](C)N[C@@H](C)C5)N=C4)C=C3)N1
The following data is based on the product molecular weight 428.54 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|
1: Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA,
Dishington AP, Gingipalli L, Gu C, Hawkins JL, Holmes JL, Howard T, Huang J,
Ioannidis S, Kazmirski S, Lamb ML, McGuire TM, Moore JE, Ogg D, Patel A, Pike KG,
Pontz T, Robb GR, Su N, Wang H, Wu X, Zhang HJ, Zhang Y, Zheng X, Wang T.
Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway
inhibitors suitable for in vivo pharmacology. ACS Med Chem Lett. 2015 Jan
13;6(3):254-9. doi: 10.1021/ml5003663. eCollection 2015 Mar 12. PubMed PMID:
25815142; PubMed Central PMCID: PMC4360163.