Blog of Signaling Pathways

Linifanib is a structurally novel potent inhibitor of RTK

3316 views | Mar 03 2014

Linifanib shows inhibitory to Kit, PDGFRβ and Flt4 with IC50 of 14 nM, 66 nM and 190 nM in kinases assay. [Read the Full Post]

Lenalidomide is effective in induring complete response

2500 views | Feb 28 2014

Lenalidomide (Revlimid, CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM. [Read the Full Post]

Deforolimus is a small molecule inhibitor of the mammalian target

2104 views | Feb 27 2014

Ridaforolimus is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. [Read the Full Post]

AZD2281 is an experimental chemotherapeutic agent

3837 views | Feb 27 2014

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM [Read the Full Post]

E7080 is a multi kinase inhibitor that is being investigated for the treatment of various

3648 views | Feb 27 2014

E7080 (Lenvatinib) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β. Phase 3. [Read the Full Post]

BCL 2 inhibition with ABT 737 prolongs survival in an NRAS

2317 views | Feb 26 2014

ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM [Read the Full Post]

Here we assess the in vitro and in vivo anti MM activity of MLN8237

2498 views | Feb 26 2014

MLN8237 shows >200-fold higher selectivity for Aurora A than the structurally related Aurora B with an IC50 of 396.5 nM, and does not have any significant activity against 205 other kinases. [Read the Full Post]

PCI 24781 is a broad spectrum hydroxamic acid based inhibitor of HDAC

3825 views | Feb 25 2014

HDAC activity is measured using a continuous trypsin-coupled assay. [Read the Full Post]

Roscovitine is an experimental drug in the family

2123 views | Feb 25 2014

Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM. [Read the Full Post]

FTY720 is a first in class orally bioavailable

2399 views | Feb 24 2014

The inhibitory effect of S1P is revered by various concentrations of FTY720. [Read the Full Post]

PP242 is a new small molecule protein inhibitor

2124 views | Feb 24 2014

PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ [Read the Full Post]

BGJ398 is a potent and selective FGFR inhibitor for FGFR

3763 views | Feb 21 2014

BGJ398 also prevents VEGFR2 with low potency. [Read the Full Post]

RAF265 is a potent selective inhibitor of C Raf

2393 views | Feb 21 2014

RAF265 shows 71% to 72% TVI% (tumor volume inhibition percentage) in HCT116 xenografts at 12 mg/kg. [Read the Full Post]

Linifanib is a structurally novel potent inhibitor of receptor tyrosine kinases

3319 views | Feb 20 2014

Linifanib shows inhibitory to Kit, PDGFRβ and Flt4 with IC50 of 14 nM, 66 nM and 190 nM in kinases assay. [Read the Full Post]

XL765 are frequently activated in human tumors

2137 views | Feb 20 2014

SAR245409 (XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. [Read the Full Post]

Dovitinib is currently under clinical investigation for hepatocellular carcinoma

3677 views | Feb 19 2014

Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 of 25 nM. [Read the Full Post]

MLN9708 is a proteasome inhibitor and is the first to enter clinical trials

3389 views | Feb 19 2014

MLN9708 is a selective, orally bioavailable, second-generation proteasome inhibitor. [Read the Full Post]

Cediranib is currently in double blind studies for the treatment

3540 views | Feb 18 2014

Cediranib (AZD2171) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM [Read the Full Post]

ARQ197 is a staurosporine derivative that binds to the dephosphorylated MET kinase

2607 views | Feb 18 2014

Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM, little activity to Ron, and no inhibition to EGFR. [Read the Full Post]

Abt199 is designed to block the function of the protein Bcl2

2658 views | Feb 14 2014

ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. [Read the Full Post]