ChemicalBook CAS DataBase List 944547-46-0

944547-46-0

Name	Mycro3
CAS	944547-46-0
Molecular Formula	C24H17ClF2N6O4
MDL Number	MFCD03409284
Molecular Weight	526.88
MOL File	944547-46-0.mol

Chemical Properties

density	1.53±0.1 g/cm3(Predicted)
storage temp.	Sealed in dry,Store in freezer, under -20°C
solubility	DMSO : ≥ 100 mg/mL (189.80 mM)
form	Solid
pka	6.95±0.46(Predicted)
color	Light yellow to yellow
InChIKey	YPPNLSKYXDXQGD-UHFFFAOYSA-N
SMILES	N1(C2=CC=CC=C2)C(NC(C2C=C3N(N=2)C(C(Cl)(F)F)=CC(C2=CC=CO2)=N3)=O)=C(C(OCC)=O)C=N1

Hazard Information

Uses

Mycro 3 is an orally active, potent and selective inhibitor of Myc-associated factor X (MAX) dimerization. Mycro 3 also inhibit DNA binding of c-Myc[1]. Mycro 3 could be used for the research of pancreatic cancer[2].

Biological Activity

Mycro 3 is a potent selective Myc-Max dimerization inhibitor. It can be used in pancreatic cancer research.

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). It has a superior specificity profile to its predecessors. It inhibits the interaction between c-Myc and Max. It has high selectivity and inhibits c-Myc/Max dimerization and conjugation with DNA.

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^[2].

Animal Model:	Moribund Pdx1-cre/KRAS* mice bearing pancreatic ductal adenocarcinoma (PDA)^[2]
Dosage:	100 mg/kg
Administration:	Oral administration; daily for two months
Result:	Increased survival time. Mycro 3 administration was discontinued after two months, the mouse survived for an additional month.

target

Myc-MAX dimerization

storage

Store at -20°C

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. DOI:10.7150/ijbs.10190
[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. DOI:10.1093/jnci/dju320

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