| CP-724714HER2 inhibitor,potent and selective |
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
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- Purity = 98.00%
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- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | CP-724714 is an inhibitor of erbB2 and EGFR kinases with IC50 values of 10±3 nM and 6,400±2,100 nM, respectively. | |||||
| Targets | erbB2 | EGFR | ||||
| IC50 | 10±3 nM | 6,400±2,100 nM | ||||
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| Cas No. | 537705-08-1 | SDF | Download SDF |
| Chemical Name | 2-methoxy-N-[(E)-3-[4-[3-methyl-4-(6-methylpyridin-3-yl)oxyanilino]quinazolin-6-yl]prop-2-enyl]acetamide | ||
| Canonical SMILES | CC1=NC=C(C=C1)OC2=C(C=C(C=C2)NC3=NC=NC4=C3C=C(C=C4)C=CCNC(=O)COC)C | ||
| Formula | C27H27N5O3 | M.Wt | 469.53 |
| Solubility | ≥23.5mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A 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. | ||
CP-724714 is an inhibitor of erbB2 and EGFR kinases with IC50 values of 10±3 nmol/L and 6,400±2,100 nmol/L, respectively [1].
In the in vitro cell cycle assay, CP-724714 cause a G1 block ofthe Her2-amplified BT-474 breast cancer cells due to its inhibition of erbB2. CP-724714 at 1 mol/L can also reduce the level of phospho-erbB2 in these cells. In in vivo assay, CP-724714 cause a concentration-dependent reduction of tumor erbB2 receptor phosphorylation in athymic mice bearing FRE-erbB2
Xenografts. CP-724714 treatments also resulted in a time- and dose-dependent induction of tumor cell apoptosis. In two human breast carcinoma models, BT-474 and MDA-MB-453, which are Her2 amplified and highly overexpress erbB2, CP-724714 is found to produce a dose-dependent inhibition of xenograft growth. In addition, CP-724,714 treatments induce reduction of downstream erbB2 RTK signaling. On the basis of these, CP-724,714 was advanced to phase I clinical trials and is potentially another option for Her2-driven breast cancer [1].
References:[1] Jitesh P. Jani, Richard S. Finn, Mary Campbell, et al. Discovery and Pharmacologic Characterization of CP-724714, a Selective ErbB2 Tyrosine Kinase Inhibitor. Cancer Research. 2007 (67): 9887-9893.
