Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C17H17N7 |
| Molecular Weight | 319.3638 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=C2C(=NN(C3CCCC3)C2=NC=N1)C4=CC5=C(NC=C5)N=C4
InChI
InChIKey=NVRXTLZYXZNATH-UHFFFAOYSA-N
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)
| Molecular Formula | C17H17N7 |
| Molecular Weight | 319.3638 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26235881 | https://www.ncbi.nlm.nih.gov/pubmed/26056008
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26235881 | https://www.ncbi.nlm.nih.gov/pubmed/26056008
PP121 is a multitargeted dual receptor tyrosine kinases inhibitor. PP121 blocks the proliferation of tumor cells by direct inhibition of oncogenic tyrosine kinases and phosphatidylinositol-3-OH kinases. PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM. PP121 blocks the proliferation of tumor cells by direct inhibition of oncogenic tyrosine kinases and phosphatidylinositol-3-OH kinases.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2041 |
|||
Target ID: CHEMBL5914 |
30.0 nM [IC50] | ||
Target ID: CHEMBL279 |
12.0 nM [IC50] | ||
Target ID: CHEMBL3234 |
8.0 nM [IC50] | ||
Target ID: CHEMBL2842 |
13.0 nM [IC50] | ||
Target ID: CHEMBL2096980 |
2.0 nM [IC50] | ||
Target ID: CHEMBL267 |
14.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
Sample Use Guides
PP121 potently and dose-dependently (0.040 to 10 uM) blocked the phosphorylation of Akt, p70S6K and S6 in two glioblastoma cell lines, U87 and LN229. PP-121 at a low concentration of 40 nM inhibits Ret autophosphorylation in TT thyroid carcinoma cells that express the C634W oncogenic Ret mutant 35. PP-121 inhibits cell proliferation with IC50 of 50 nM in TT thyroid carcinoma cells. PP-121 inhibits cell proliferating stimulated only with VEGF with IC50 of 41 nM in human umbilical vein endothelial cells (HUVECs).
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:47:21 UTC 2023
by
admin
on
Fri Dec 15 16:47:21 UTC 2023
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| Record UNII |
5B9VB06146
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| Record Status |
Validated (UNII)
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| Record Version |
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5B9VB06146
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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INHIBITOR -> TARGET | |||
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TARGET -> INHIBITOR |
