| 10074-G5c-Myc inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
10074-G5 Dilution Calculator
calculate
10074-G5 Molarity Calculator
calculate
| Cas No. | 413611-93-5 | SDF | Download SDF |
| Chemical Name | N-[1,1"-biphenyl]-2-yl-7-nitro-2,1,3-benzoxadiazol-4-amine | ||
| Canonical SMILES | O=[N+](C(C1=NON=C12)=CC=C2NC3=CC=CC=C3C4=CC=CC=C4)[O-] | ||
| Formula | C18H12N4O3 | M.Wt | 332.3 |
| Solubility | ≤2mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
10074-G5 is a c-Myc inhibitor [1].
c-Myc is a bHLH-ZIP transcription factor involved in cell cycle progression, cellular growth and metabolism, differentiation, and apoptosis. Overexpression of c-Myc has been identified in numerous cancers, including prostate, pancreatic, lung, breast, and colon cancers, B-cell lymphoma, and leukemias. Alterations in c-Myc have been associated with cancer aggressiveness and poor treatment prognosis. Inhibition of c-Myc is an attractive pharmacological approach in the development of new anticancer treatments. Inactivation of c-Myc rapidly results in cell-cycle arrest, apoptosis, tumor vascular degeneration, redifferentiation of tumor cells, and ultimately tumor regression [1].
The IC50 values of 10074-G5 against Daudi cells and HL-60 cells were 15.6 ± 1.5 μM and 13.5 ± 2.1 μM, respectively. 10074-G5 (10 μM) inhibited c-Myc/Max dimerization and decreased total c-Myc protein expression. In C.B-17 SCID mice bearing Daudi xenografts, treatment with 10074-G5, (20 mg/kg i.v., for 10 consecutive days) significantly inhibited tumor growth with no effects on body weight.
References:[1] Clausen D M, Guo J, Parise R A, et al. In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization[J]. Journal of Pharmacology and Experimental Therapeutics, 2010, 335(3): 715-727.
