Blog of Signaling Pathways

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

3504 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

2230 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

2387 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

3648 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

2047 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

2272 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

2035 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

3600 views | Feb 21 2014

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

RAF265 is a potent selective inhibitor of C Raf

2321 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

3194 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

2063 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

3524 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

3253 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

3407 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

2464 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

2569 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]

XL184 is a small molecule inhibitor of the tyrosine kinases

3140 views | Feb 14 2014

XL184 has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM [Read the Full Post]

SB431542 is a small molecule that acts as a specific inhibitor

3580 views | Feb 13 2014

SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases. [Read the Full Post]

RO4929097 is a small molecule gamma secretase inhibitor

3224 views | Feb 13 2014

RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. [Read the Full Post]

SB525334 is a potent and selective inhibitor of TGFB

3444 views | Feb 12 2014

SB 525334 (10 mg/kg/day) decreases the renal mRNA levels of PAI-1, procollagen α1(I), and procollagen α1(III) in a nephritis-induced renal fibrosis rat model. [Read the Full Post]