Mycro 3

Mycro 3 is a potent and selective inhibitor of Myc-associated factor X (MAX) dimerization. Mycro 3 also inhibit DNA binding of c-Myc. Mycro 3 could be used for the research of pancreatic cancer.

Product information

CAS Number: 944547-46-0

Molecular Weight: 526.88

Formula: C24H17ClF2N6O4

Chemical Name: ethyl 5-[7-(chlorodifluoromethyl)-5-(furan-2-yl)pyrazolo[1, 5-a]pyrimidine-2-amido]-1-phenyl-1H-pyrazole-4-carboxylate

Smiles: CCOC(=O)C1C=NN(C2=CC=CC=C2)C=1NC(=O)C1C=C2N=C(C=C(N2N=1)C(F)(F)Cl)C1=CC=CO1

InChiKey: YPPNLSKYXDXQGD-UHFFFAOYSA-N

InChi: InChI=1S/C24H17ClF2N6O4/c1-2-36-23(35)15-13-28-32(14-7-4-3-5-8-14)21(15)30-22(34)17-12-20-29-16(18-9-6-10-37-18)11-19(24(25,26)27)33(20)31-17/h3-13H,2H2,1H3,(H,30,34)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : ≥ 100 mg/mL (189.80 mM)

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: ≥360 days 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:

Mycro 3 is a potent and selective c-Myc inhibitor in whole cell assays, with weak inhibitory activity against Activator protein 1 (AP-1). Mycro 3 has a superior specificity profile to its predecessors. Mycro 3 inhibits the interaction between c-Myc and Max. Mycro 3 has high selectivity and inhibits c-Myc/Max dimerization and conjugation with DNA[1]. Mycro 3 exhibits an excellent specificity with IC50s of 0.25 and 9.0 µM for cells with intact Myc alleles and Myc-null cells, respectively.

In Vivo:

Mycro 3 (100 mg/kg; oral administration; daily for two months) induces marked shrinkage of pancreatic ductal adenocarcinoma (PDA), increases cancer cell apoptosis, and reduces cell proliferation. Tumor growth is also drastically attenuated in Mycro 3-treated NOD/SCID mice carrying orthotopic or heterotopic xenografts of human pancreatic cancer cells.

References:

1. Chen BJ, et al. Small molecules targeting c-Myc oncogene: promising anti-cancer therapeutics. Int J Biol Sci. 2014 Sep 13;10(10):1084-96.
2. Dimitris Stellas, et al. Therapeutic effects of an anti-Myc drug on mouse pancreatic cancer. J Natl Cancer Inst. 2014 Oct 11;106(12):dju320.

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