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PP121 CAS: 1092788-83-4

Category: Inhibitors
Product Name: PP121
Cat No: I000387
CAS No: 1092788-83-4
Synonyms: PP121; 1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazolo[3,4-d]pyrimidin-4-amine
Molecular Formula: C17H17N7
Molecular Weight: 319.4
SMILES: NC1=C(C(C2=CN=C(NC=C3)C3=C2)=NN4C5CCCC5)C4=NC=N1
InChI: InChI=1S/C17H17N7/c18-15-13-14(11-7-10-5-6-19-16(10)20-8-11)23-24(12-3-1-2-4-12)17(13)22-9-21-15/h5-9,12H,1-4H2,(H,19,20)(H2,18,21,22)
InChIKey: NVRXTLZYXZNATH-UHFFFAOYSA-N
Solubility: DMSO ≥61mg/mL Water <1.2mg/mL Ethanol ≥1.8mg/mL
Target: PI3K
CAS 1092788-83-4,PP121
  • Description

PP121(cas# 1092788-83-4) is dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR). PP121 exhibits no significant effect on receptor serine/threonine kinases (RSTKs). PP121 blocks the proliferation of tumor cells by direct inhibition of PI 3-K, mTOR, Src and the VEGF receptor.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References

1. Biochem Biophys Res Commun. 2015 Sep 11;465(1):137-44. doi: 10.1016/j.bbrc.2015.07.147. Epub 2015 Jul 30.
The anti-esophageal cancer cell activity by a novel tyrosine/phosphoinositide kinase inhibitor PP121.
Peng Y(1), Zhou Y(1), Cheng L(2), Hu D(3), Zhou X(3), Wang Z(3), Xie C(4), Zhou F(5).
Author information:
(1)Department of Radiation and Medical Oncology, Hubei Key Laboratory of Tumor Biological Behaviors, Zhongnan Hospital of Wuhan University, Wuhan 430071, China; Department of Radiation Oncology, Hubei Cancer Hospital, Wuhan 430071, China. (2)Department of Interventional Radiology, the Second Affiliated Hospital of Soochow University, Soochow University, Suzhou 215001, China. (3)Department of Radiation Oncology, Hubei Cancer Hospital, Wuhan 430071, China. (4)Department of Radiation and Medical Oncology, Hubei Key Laboratory of Tumor Biological Behaviors, Zhongnan Hospital of Wuhan University, Wuhan 430071, China. Electronic address: chxie_65@hotmail.com. (5)Department of Radiation and Medical Oncology, Hubei Key Laboratory of Tumor Biological Behaviors, Zhongnan Hospital of Wuhan University, Wuhan 430071, China. Electronic address: ZhouFuxiangwuhan@126.com.
Here we explored the potential effect of PP121, a novel dual inhibitor of tyrosine and phosphoinositide kinases, against human esophageal cancer cells. We showed that PP121 exerted potent cytotoxic effect in primary (patient-derived) and established (Eca-109, TE-1 and TE-3 lines) esophageal cancer cells, possibly through activating caspase-3-dependnent apoptosis. PP121 was, however, non-cytotoxic to the normal human esophageal epithelial cells (EECs). At the molecular level, we showed that PP121 blocked Akt-mTOR (mammalian target of rapamycin) activation in esophageal cancer cells, which was restored by introducing a constitutively-active Akt (CA-Akt). Yet, CA-Akt only partly inhibited cytotoxicity by PP121 in Eca-109 cells. Importantly, we showed that PP121 inhibited nuclear factor kappa B (NFκB) signaling activation in esophageal cancer cells, which appeared independent of Akt-mTOR blockage. In vivo, oral administration of PP121 remarkably inhibited Eca-109 xenograft growth in nude mice, and significantly improved mice survival. Further, the immunohistochemistry (IHC) and Western blot assays analyzing xenografted tumors showed that PP121 inhibited Akt-mTOR and NFκB activations in vivo. Together, we demonstrate that PP121 potently inhibits esophageal cancer cells in vitro and in vivo, possibly through concurrently inhibiting Akt-mTOR and NFκB signalings.
2. Tumour Biol. 2014 Sep;35(9):8659-64. doi: 10.1007/s13277-014-2118-3. Epub 2014 May 28.
PP121, a dual inhibitor of tyrosine and phosphoinositide kinases, inhibits anaplastic thyroid carcinoma cell proliferation and migration.
Che HY(1), Guo HY, Si XW, You QY, Lou WY.
Author information:
(1)Shaoxing People's Hospital, Shaoxing Hospital of Zhejiang University, 568 Zhongxing North Road, Shaoxing, Zhejiang, 312000, People's Republic of China.
The tyrosine and phosphoinositide kinases play crucial roles in the regulation of many cancer cell processes including cell survival and cell motility. Anaplastic thyroid carcinoma (ATC) is a rare and deadly type of thyroid cancer, and so far, there are no effective therapeutic compounds for ATC. Herein, we investigate the anticancer activities of PP121, a dual inhibitor of tyrosine and phosphoinositide kinases, in ATC therapy. We found that PP121 is effective at suppressing cell viability, inducing cell apoptosis, and inhibiting cell migration and invasion. The potential anticancer mechanism for PP121 might be its inhibitory effects on phosphatidylinositol 3-kinase (PI3K)/Akt signaling pathways in ATC cells. Furthermore, PP121 is effective at suppressing ATC tumor growth in vivo. In summary, our studies suggest that PP121 might be a promising therapeutic compound for ATC treatment, which might shed new light on ATC therapy.


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