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1092788-83-4

1092788-83-4 structure
1092788-83-4 structure
  • Name: PP121
  • Chemical Name: 1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazolo[3,4-d]pyrimidin-4-amine
  • CAS Number: 1092788-83-4
  • Molecular Formula: C17H17N7
  • Molecular Weight: 319.364
  • Catalog: Biochemical Inhibitor Protein tyrosine kinase
  • Create Date: 2018-12-18 13:45:15
  • Modify Date: 2024-01-03 11:08:57
  • PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively.
Name 1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazolo[3,4-d]pyrimidin-4-amine
Synonyms S2622_Selleck
PP-121,PP 121
1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
KS1
PP121
Description PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively.
Related Catalog
Target

mTOR:10 nM (IC50)

PDGFR:2 nM (IC50)

VEGFR2:12 nM (IC50)

Src:14 nM (IC50)

DNK-PK:60 nM (IC50)

In Vitro PP121 blocks the PI3K pathway by direct inhibition of PI3K/mTOR in two glioblastoma cell lines, U87 and LN229. PP121 potently inhibits the proliferation of a diverse panel of tumor cell lines containing mutations in the PI3-K pathway components PIK3CA, PTEN, or RAS. PP121 induces a G0G1 arrest in most tumor cells. PP121 directly inhibits Src in cells and reverses its biochemical and morphological effects. PP121 potently inhibits the Ret kinase domain in vitro (IC50<1 nM). PP121 potently blocks VEGF stimulated activation of the PI3-K and MAPK pathways. PP121 inhibits VEGFR2 autophosphorylation at low nanomolar concentrations, confirming that this molecule directly targets VEGFR2 in cells. PP121 inhibits Bcr-Abl induced tyrosine phosphorylation in K562 cells as well as BaF3 cells that express Bcr-Abl[1].
In Vivo Oral administration of PP121 remarkably inhibits Eca-109 xenograft growth. Mice body weights are not significantly affected by PP121 or the vehicle treatment. PP121 oral administration dramatically inhibits activations of Akt-mTOR and NFkB in xenograft tumors. p-Akt Ser 473 and p-IKKa/b are both inhibited by PP121 administration[2].
Kinase Assay Purified kinase domains are incubated with inhibitors (PP121) at 2- or 4-fold dilutions over a concentration range of 50- 0.001 µM or with vehicle (0.1% DMSO) in the presence of 10 µM ATP, 2.5 µCi of γ- 32P-ATP and substrate. Reactions are terminated by spotting onto nitrocellulose or phosphocellulose membranes, depending on the substrate; this membrane is then washed 5-6 times to remove unbound radioactivity and dried. Transferred radioactivity is quantitated by phosphorimaging and IC50 values are calculated by fitting the data to a sigmoidal doseresponse using Prism software[1].
Cell Assay Cells grown in 96-well plates are treated with PP121 at 4-fold dilutions (10 µM - 0.040 μM) or vehicle (0.1% DMSO). After 72 h cells are exposed to Resazurin sodium salt (22 µM) and fluorescence is quantified. IC50 values are calculated. For proliferation assays involving single cell counting, non-adherent cells are plated at low density (3–5% confluence) and treated with drug (2.5 µM) or vehicle (0.1% DMSO). Cells are diluted into trypan blue daily and viable cells counted using a hemocytometer[1].
Animal Admin Mice: Eca-109 cells are injected into the axillary regions of nude mice (5×106 cells/mouse). When the tumor volumes reach around 200 mm3, the mice are randomly separated to three groups: Untreated control, PP121 (30 mg/kg) and vehicle (10% 1-methyl-2-pyrrolidinone and 90% PEG 300) group. Tumor volumes and the mice body weights are measured every 10 d[2].
References

[1]. Apsel B, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol, 2008, 4(11), 691-699.

[2]. Peng Y, et al. The anti-esophageal cancer cell activity by a novel tyrosine/phosphoinositide kinase inhibitor PP121. Biochem Biophys Res Commun. 2015 Sep 11;465(1):137-44.

Density 1.63
Boiling Point 650.9±50.0 °C at 760 mmHg
Molecular Formula C17H17N7
Molecular Weight 319.364
Flash Point 347.4±30.1 °C
Exact Mass 319.154541
PSA 98.30000
LogP 2.41
Appearance off-white
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.881
Storage condition Store at +4°C
Water Solubility DMSO: >10mg/mL
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Hazard Codes Xn
Risk Phrases 22
RIDADR UN 2811 6.1 / PGIII
Hazard Class 22
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