- CEP-32496
- Vemurafenib (PLX4032, RG7204)
- Sorafenib
- PLX-4720
- BRAF inhibitor
| AZ 628Raf kinases,potent and ATP-competitive |
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 | AZ628 is a new inhibitor of BRAF, BRAFV600E and c-Raf-1 with IC50 values of 105 nM, 34 nM and 29 nM,respectively. | |||||
| Targets | C-Raf-1 | B-Raf (V600E) | B-Raf | |||
| IC50 | 29 nM | 34 nM | 105 nM | |||
AZ 628 Dilution Calculator
calculate
AZ 628 Molarity Calculator
calculate
| Cas No. | 878739-06-1 | SDF | Download SDF |
| Synonyms | AZ-628; AZ628 | ||
| Chemical Name | 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxoquinazolin-6-yl)amino]phenyl]benzamide | ||
| Canonical SMILES | CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(C)(C)C#N)NC3=CC4=C(C=C3)N=CN(C4=O)C | ||
| Formula | C27H25N5O2 | M.Wt | 451.53 |
| Solubility | ≥22.6mg/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. | ||
AZ628 is a potent and newly discorvered inhibitor of BRAF, c-Raf-1 and BRAFV600E with IC50 values of 105 nM, 29 nM and 34 nM, respectively. This compound prevents CRAF activation through persistently occupying the ATP-binding site of Raf kinase. Specificity profile suggests that AZ628 also inhibits activation of other tyrosine protein kinases such as DDR2, VEGFR2, Lyn, Flt1, FMS and others.
Raf kinases a family of three serine/threonine-specific protein kinases and participate in the RAS-RAF-MEK-ERK signal transduction cascade, also known as the mitogen-activated protein kinase (MAPK) cascade. The activation of MAPK signaling leads to different cellular response such as cell proliferation, apoptosis and inflammation.
AZ628 has the potent anti-tumor activity. In human colon and melanoma-derived cell line that carries the recurrent V600E activating BRAF mutation, AZ628 was shown to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis [1]. AZ628 may be antiangiogenic due to inhibition of VEGFR2 [2].
Generation of melanoma cell line clones is obtained resistance to the RAF kinase inhibitor AZ628. Resistance to AZ628 is connected with raised levels of the RAF downstream effector p-ERK1/2. ERK1/2 initiation in AZ628-resistant clones is interceded by MEK. Supported multiplication of AZ628-resistant clones is to a great extent autonomous of BRAF kinase action. AZ628-resistant clones express elevated CRAF. Survival of AZ628-safe cells is subject to CRAF [1].
References:1. Montagut C, Sharma SV, Shioda T, McDermott U, Ulman M, Ulkus LE, et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res 2008,68:4853-4861.2. Khazak V, Astsaturov I, Serebriiskii IG, Golemis EA. Selective Raf inhibition in cancer therapy. Expert Opin Ther Targets 2007,11:1587-1609.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
>
搞核酸的：PCR仪器，电泳槽，电泳仪，凝胶扫描设备
搞蛋白的：各类电泳设备，转膜仪，摇床，有需要还要特别搞一个暗房间
基本就这些吧，话说，兄台真要筹建一个实验室，为何不亲自到一个实验室转一圈呢？
