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  1. General Info
  2. Effects Info
  3. Reference
Drug Details
01. General Information
Name PP242
PubChem CID 135565635
Molecular Weight 308.34g/mol
Synonyms

PP242, 1092351-67-1, TORKinib, PP-242, PP 242, 2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, Torkinib (PP242), 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol, H5669VNZ7V, DTXSID5048685, CHEBI:90679, 2-(4-Amino-1-isopropyl-1H-pyrazolo(3,4-d)pyrimidin-3-yl)-1H-indol-5-ol, 2-[4-Amino-1-(Propan-2-Yl)-1h-Pyrazolo[3,4-D]pyrimidin-3-Yl]-1h-Indol-5-Ol, 1H-Indol-5-ol, 2-(4-amino-1-(1-methylethyl)-1H-pyrazolo(3,4-d)pyrimidin-3-yl)-, 2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo-[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol, DTXCID5028611, CAS-1092351-67-1, UNII-H5669VNZ7V, EX-7207, Torkinib (PP242)?, MLS006011184, SCHEMBL298922, GTPL5704, CHEMBL1241674, CHEMBL3988893, SCHEMBL21381567, BDBM36409, CHEBI:95099, EX-A034, MFAQYJIYDMLAIM-UHFFFAOYSA-N, HMS3655B12, AMY23716, BCP02319, Tox21_113072, 2-{4-amino-1-isopropylpyrazolo[3,4-d]pyrimidin-3-yl}-1H-indol-5-ol, MFCD12196869, NSC764515, s2218, AKOS024458060, AKOS026750472, Tox21_113072_1, CCG-267563, CS-0247, NSC-764515, (2E)-2-(4-amino-1-propan-2-yl-2H-pyrazolo[3,4-d]pyrimidin-3-ylidene)indol-5-ol, CID24905147, NCGC00188346-02, NCGC00188346-03, NCGC00188346-18, NCGC00387863-04, AC-28392, AS-16317, HY-10474, SMR004702953, FT-0696781, SW220211-1, A25462, J-507663, BRD-K87112191-001-02-9, Q27088430, Q27166867, 2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indole-5-ol, 2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, (2E)-2-(4-amino-1-propan-2-yl-2H-pyrazolo[3, 4-d]pyrimidin-3-ylidene)indol-5-ol, 2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, PP242, 2-(4-amino-1-propan-2-yl-2H-pyrazolo[3,4-d]pyrimidin-3-ylidene)-5-indolol, P2X

Drug Type Small molecule
Formula C₁₆H₁₆N₆O
SMILES CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N
InChI 1S/C16H16N6O/c1-8(2)22-16-13(15(17)18-7-19-16)14(21-22)12-6-9-5-10(23)3-4-11(9)20-12/h3-8,20,23H,1-2H3,(H2,17,18,19)
InChIKey MFAQYJIYDMLAIM-UHFFFAOYSA-N
CAS Number 1092351-67-1
ChEMBL ID CHEMBL3988893
ChEBI ID CHEBI:90679
Toxicity Organism Test Type Route(Dose)
Structure 2D-img
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2D MOL 3D MOL
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 551
Pair Name Sulforaphane, PP242
Partner Name Sulforaphane
Disease Info [ICD-11: 2B70] Esophageal cancer Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Down-regulation Phosphorylation AKT1 hsa207
Down-regulation Phosphorylation AKT1S1 hsa84335
Up-regulation Expression BAX hsa581
Up-regulation Cleavage CASP9 hsa842
Down-regulation Phosphorylation RICTOR hsa253260
Down-regulation Phosphorylation RPS6KB1 hsa6198
In Vitro Model Eca-109 Esophageal squamous cell carcinoma Homo sapiens (Human) CVCL_6898
EC9706 Esophageal squamous cell carcinoma Homo sapiens (Human) CVCL_E307
Result Our findings demonstrate that PP242 enhances the anti-tumor activity of SFN by blocking SFN-induced activation of Akt/mTOR pathway in ESCC, which provides a rationale for treating ESCC using SFN combined with Akt/mTOR pathway inhibitors.
03. Reference
No. Title Href
1 mTOR inhibitor PP242 increases antitumor activity of sulforaphane by blocking Akt/mTOR pathway in esophageal squamous cell carcinoma. Mol Biol Rep. 2022 Jan;49(1):451-461. doi: 10.1007/s11033-021-06895-9. Click
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