Products

A cell-permeable indenopyrazole compound that displays potent antiproliferativeproperties in several human

tumor cell lines (IC₅₀ <33 nM). Shown to act as an ATP-competitive and reversible inhibitor of PDGFR (IC₅₀=

4.2 nM and 45 nM for -β and -α, respectively) and c-Abl (IC₅₀ = 22 nM).Exhibits less activity towards Lck, c-Src,

and Fyn(IC₅₀ = 100 nM, 185 nM and 378 nM, respectively) and exhibits little or noinhibition toward VEGFR, HER-2,

Cdk's-1,-2,-4 &-7, bFGFR-1 and EGFR (IC₅₀ = 3.1 µM, >10 µM, >10 µM, 45.8 µM and >100 µM, respectively).

A cell-permeable pyridopyrimidine compound that acts as a potent, ATP-competitive, and reversible inhibitor of

FGF and VEGF receptors (IC₅₀ = 21.5 nM for FGFR1). It inhibits PDGFR and c-Src only at muchhigher

concentration (IC₅₀ = 17.6 µM, 19.8 µM, respectively) and exhibits little effect against EGFR, InsR, MEK, andcPKC

even at concentrations as high as 50 µM. Shown to inhibit the autophosphorylation of endogenous FGFR1 (IC₅₀

<5 nM) and overexpressed VEGFR2 (IC₅₀ <200 nM) in NIH3T3 cells in vitro, and FGF- andVEGF-induced

angiogenesis in mice in vivo.

A cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck,

and Src (IC₅₀ = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinasessuch as CSK, RIP2, and

CK1δ (IC₅₀ = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 µM, in vitro kinaseactivity is

reduced by more than 57% for p38α, p38β, CK1δ, CSK, RIP2, and GAK, while exhibiting muchlower activity

against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr4:1] indicate that the

inhibition is mixed competitive with respect to the substrate and non-competitive with respect toATP. PP1 also

demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC₅₀= 2.5 to

8.0 µM) and pediatric brain tumor cells (IC₅₀ = 1.1 to 9.7 µM).

A cell-permeable pyrazolopyrimidinecompound that effectively targets the ATP pocket of both protein tyrosine

kinases (IC₅₀ <0.26 μM against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, Src, andVEGFR2) and PI3-K T338I

family kinases (IC₅₀ <1.4 μM against p110α/β/δ/γ, mTOR, and DNA-PK).PP121 is less effective against ser/thr

kinases and exhibits significant inhibition of only 14 ser/thr kinases (≥70% inhibition with 1 μM inhibitor and 10 mM

ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC₅₀ = 780 nM) or PI3-K/mTOR

pathway by PI-103 (IC₅₀ = 800 nM) is shown to be less effective than PP121 treatment (IC₅₀ = 50 nM) in inhibiting

the proliferation of Ret C634W-expressing TT thyroid carcinoma cultures. 

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit

(IC₅₀ = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC₅₀= 7.0 µM

and 7.3 µM). Also displays antiangiogenic and antitumor properties. Does not inhibit the activities ofCDK-1,

c-Met, IGF-1R or PKA (IC₅₀ > 10 µM).

Catalog No.

Product Name

Size

CD0165

PDGFR Tyrosine Kinase Inhibitor IV

(RWJ 540973, JNJ-10198409)

1mg, 5mg, 10mg, 25mg

& 50mg

CD0172

PD173074 – FGF/VEGFReceptor

Tyrosine Kinase Inhibitor

1mg, 5mg, 10mg, 25mg,

50mg, 100mg, 200mg,

250mg, 500mg & 1g

CD0334

PP1 – Src Inhibitor

1mg, 5mg, 10mg, 25mg,

50mg & 100mg

CD0257

pp121 – Tyrosin Kinase and PI3K Pathway Inhibitor

1mg, 5mg, 10mg, 25mg,

50mg ,100mg & 200mg

CD0207

VEGFR Tyrosine Kinase Inhibitor II

1mg, 5mg, 10mg, 25mg, 

50mg & 100mg