In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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 . AZ628 may be antiangiogenic due to inhibition of VEGFR2 .
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. 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.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥22.6mg/mL in DMSO|
|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.|
|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.|
|IC50||29 nM||34 nM||105 nM|