DiscoveryProbe™ Tyrosine Kinase/Adaptors-related Compounds Panel

Compound Panel Contents

Catalog No.	Product Name	Summary	Targets	CAS Number	Smiles
A8328	LDK378	Potent ALK inhibitor	Tyrosine Kinase/Adaptors|ALK	1032900-25-6	CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl
B1402	GZD824	Bcr-Abl inhibitor,novel orally bioavailable	Tyrosine Kinase/Adaptors|Bcr-Abl	1421783-64-3	CC1=CC=C(C(NC2=CC=C(CN3CCN(C)CC3)C(C(F)(F)F)=C2)=O)C=C1C#CC4=CN=C5C(C=NN5)=C4.CS(=O)(O)=O.CS(=O)(O)=O
A2838	OSI-930	Potent inhibitor of Kit, KDR, Flt, CSF-1R, c-Raf and Lck	Tyrosine Kinase/Adaptors|c-Kit	728033-96-3	C1=CC=C2C(=C1)C(=CC=N2)CNC3=C(SC=C3)C(=O)NC4=CC=C(C=C4)OC(F)(F)F
A1196	SGX-523	MET inibitor, highly selective, ATP-competitive	Tyrosine Kinase/Adaptors|c-MET	1022150-57-7	CN1C=C(C=N1)C2=NN3C(=NN=C3SC4=CC5=C(C=C4)N=CC=C5)C=C2
A2977	Cabozantinib (XL184, BMS-907351)	VEGFR2/Met/Ret/Kit/FLT//AXL inhibitor	Tyrosine Kinase/Adaptors|c-MET	849217-68-1	COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F
A8320	PF-00562271	FAK/Pyk2 inhibitor,potent and ATP-competitive	Tyrosine Kinase/Adaptors|FAK	939791-38-5	CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C.C1=CC=C(C=C1)S(=O)(=O)O
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Advantages

• Available in stock with overnight delivery and free shipping over $500
• Cost-effective and competitive price to save your findings
• Potent, selective and cell-permeable in inhibiting or activating target molecules
• Diverse in chemical structure and route of administration (oral/i.m/i.v injection etc.)
• Detailed files describing potency, selectivity and applications etc.
• Supported by published data from top peer-reviewed journals
• Guaranteed high quality with NMR and HPLC validation

产品描述
A wide range of well-characterized bioactive molecules that covers various targets related to tyrosine kinase/adaptors, including ALK, c-MET, VEGFR and Src etc. Facilitate your research towards the insights of cancer, immune response, growth and differentiation etc. Applicable in cellular assays, animal models and drug screenings etc.
References
1. Lemmon MA, Schlessinger J. Cell signaling by receptor tyrosine kinases. Cell. 2010 Jun 25;141(7):1117-34. 
Abstract 
Recent structural studies of receptor tyrosine kinases (RTKs) have revealed unexpected diversity in the mechanisms of their activation by growth factor ligands. It provides an important context for therapeutically countering the effects of pathogenic RTK mutations in cancer and other diseases. Much remains to be learned, however, about the complex signaling networks downstream from RTKs and how alterations in these networks are translated into cellular responses.
2. Wang Y, Wang L, Guan S et al.Novel ALK inhibitor AZD3463 inhibits neuroblastoma growth by overcoming crizotinib resistance and inducing apoptosis. Sci Rep. 2016 Jan 20;6:19423. 
Abstract 
ALK receptor tyrosine kinase has been shown to be a therapeutic target in neuroblastoma. In this study, we show that a new ALK inhibitor AZD3463 effectively suppressed the proliferation of NB cell lines with wild type ALK (WT) as well as ALK activating mutations (F1174L and D1091N) by blocking the ALK-mediated PI3K/AKT/mTOR pathway and ultimately induced apoptosis and autophagy. In addition, AZD3463 not only enhanced the cytotoxic effects of doxorubicin on NB cells but also exhibited significant therapeutic efficacy on the growth of the NB tumors with WT and F1174L activating mutation ALK in orthotopic xenograft mouse models. These results indicate that AZD3463 is a promising therapeutic agent in the treatment of NB.