| AZD2932inhibitor of VEGFR-2, PDGFRβ, Flt-3, and c-Kit |
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
AZD2932 Dilution Calculator
calculate
AZD2932 Molarity Calculator
calculate
| Cas No. | 883986-34-3 | SDF | Download SDF |
| Chemical Name | (Z)-2-(4-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-N-(1-isopropyl-1H-pyrazol-4-yl)acetimidic acid | ||
| Canonical SMILES | CC(N1C=C(/N=C(O)/CC2=CC=C(OC3=NC=NC4=CC(OC)=C(OC)C=C43)C=C2)C=N1)C | ||
| Formula | C24H25N5O4 | M.Wt | 447.49 |
| Solubility | Soluble in DMSO | 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. | ||
AZD2932 is a potent inhibitor for multiple protein tyrosine kinases (IC50 = 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.) [1]
VEGFR are receptors for vascular endothelial growth factor and belong to receptor tyrosine kinases. It mediates in various cellular functions, including endothelial proliferation, migration, survival, tubular morphogenesis and sprouting. PDGFR are platelet-derived growth factor receptors that exhibit intracellular tyrosine kinase activity. It involves in embryonic development, angiogenesis, proliferation and differentiation etc.
AZD2932 has a potent and balanced profile against PDGFR, VEGFR-2, Flt-3 and c-Kit (IC50: 0.009). It also has a good fraction unbound between 3.3% free in human and 7.0% in dog sera and has no activity against hERG. [1]
In female nude mice bearing C6 tumors, AZD2932 treatment at 3–50 mg/kg b.i.d. 10 h apart give 60–80% inhibition of both p-VEGFR-2 and p-PDGFRb in a 1:1 ratio. [1]
Reference:1. Plé PA, Jung F, Ashton S, Hennequin L et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6.
