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PP121

In stock
Catalog No.
B2172
Dual inhibitor of tyrosine and phosphoinositide kinases
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
10mg
$80.00
In stock
50mg
$260.00
In stock
200mg
$680.00
In stock

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PP121 is a dual inhibitor of tyrosine and phosphoinositide kinases [1].

PP121 is found to inhibit both tyrosine kinases and PI3-Ks but not serine-threonine kinases. It potently inhibits p110α, p110β, p110γ, p110δ, DNA-PK and mTOR with IC50 values of 52nM, 1.4μM, 1.1μM, 150nM, 60nM and 10nM, respectively. For the tyrosine kinases, PP121 shows inhibition with IC50 values of 21nM, 4nM, 10nM,55nM, 550nM, 220nM and <1nM for Ab1, Hck, Src, VEGFR2, EGFR, EphB4 and PDGFR, respectively [1].

In cells, PP121 can reverse v-Src mediated cellular transformation and restore actin stress fiber staining. PP121 also potently inhibits the mutant Ret kinase with IC50 value less than 1nM in thyroid tumors34. Furthermore, PP121 is found to evade drug resistance through redundantly targeting Bcr-Abl mediated cell survival and PI3-K/mTOR mediated cell proliferation [1].

References:
[1] Apsel B, Blair J A, Gonzalez B, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nature chemical biology, 2008, 4(11): 691-699.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt319.37
Cas No.1092788-83-4
FormulaC17H17N7
Solubility≥15.95mg/mL in DMSO
Chemical Name1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazolo[3,4-d]pyrimidin-4-amine
SDFDownload SDF
Canonical SMILESC1CCC(C1)N2C3=C(C(=N2)C4=CN=C5C(=C4)C=CN5)C(=NC=N3)N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Biological Activity

Description PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 values of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM,respectively.
Targets PDGFR Hck VEGFR mTOR Src Abl
IC50 2 nM 8 nM 12 nM 13 nM 14 nM 18 nM

Quality Control

Quality Control & MSDS

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Chemical structure

PP121