- SNS-314 Mesylate
- VX-680 (MK-0457,Tozasertib)
- MK-8745
- PF-03814735
- CYC116
- Barasertib (AZD1152-HQPA)
| CCT137690Aurora A/B/C 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)
- Datasheet
Chemical structure
| Description | CCT137690 is a highly selective and orally bioavailable inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM, respectively. | |||||
| Targets | Aurora A | Aurora B | Aurora C | |||
| IC50 | 15 nM | 25 nM | 19 nM | |||
CCT137690 Dilution Calculator
calculate
CCT137690 Molarity Calculator
calculate
| Cas No. | 1095382-05-0 | SDF | Download SDF |
| Chemical Name | 3-[[4-[6-bromo-2-[4-(4-methylpiperazin-1-yl)phenyl]-1H-imidazo[4,5-b]pyridin-7-yl]piperazin-1-yl]methyl]-5-methyl-1,2-oxazole | ||
| Canonical SMILES | CC1=CC(=NO1)CN2CCN(CC2)C3=C4C(=NC=C3Br)N=C(N4)C5=CC=C(C=C5)N6CCN(CC6)C | ||
| Formula | C26H31BrN8O | M.Wt | 551.48 |
| Solubility | ≥6.9 mg/mL in DMSO, <2.63 mg/ml="" in="" etoh,=""><2.4 mg/ml="" in="" h2o=""> | 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. | ||
CCT137690 is an orally bioavailable inhibitor of aurora kinases with IC50 values in a range from 15 to 25 nM [1].
Aurora kinase is a family of serine/threonine kinases including Aurora-A, B and C. They play important roles in the regulation of mitosis and take participate in the causation and progression of various tumors including ovarian, breast, glioma and colon. Therefore aurora kinases have been regarded as anti-cancer targets in cancer chemotherapeutics.CCT137690 is a selective small-molecular inhibitor of aurora kinases and showed anti-tumor activities both in vitro and in vivo. Besides that, CCT137690 exerted good stability in mouse liver microsomes [1].
When tested toward a panel of 94 kinases, CCT137690inhibited 80% activities of VEG-FR, Aurora-A, and FGF-R1 at concentration of 1 μM. It suppressed the phosphorylation of histone H3 caused by Aurora-B. The IC50 values of CCT137690 against Aurora-B and C were 25 and 19 nM, respectively. CCT137690 showed potent anti-proliferation effects on various kinds of tumors such as A2780 ovarian tumor cell (IC50 value of 140 nM), SW620 (IC50 value of 300 nM) and SW48 colon carcinoma (IC50 value of 157 nM). It caused cell cycle perturbations. In addition, CCT137690 was found to have synergistic effects with radiotherapy. It increased the sensitivity of SW620 cells to radiation. The combination treatment resulted in much more cell death through apoptosis [1 and 2].
In mice model bearing SW620 xenografts, administration of CCT137690slowed the growth of tumors without observed toxicity. The ratio of treat/control group based on tumor weight was 37% at the dose of 75 mg/kg. Besides that, CCT137690 was found to significantly reduced neuroblastoma tumor mass in MYCN transgenic mice, which meant CCT137690 could benefit patients with MYCN-amplified neuroblastoma [1 and 3].
References:[1] Bavetsias V, Large J M, Sun C, et al. Imidazo [4, 5-b] pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. Journal of medicinal chemistry, 2010, 53(14): 5213-5228.[2] Wu X, Liu W, Cao Q, et al. Inhibition of Aurora B by CCT137690 sensitizes colorectal cells to radiotherapy. J ExpClin Cancer Res, 2014, 33(1): 13.[3] Faisal A, Vaughan L, Bavetsias V, et al. The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Molecular cancer therapeutics, 2011, 10(11): 2115-2123.
