PP242 - ≥98%, high purity , CAS No.1092351-67-1, Inhibitor of mechanistic target of rapamycin kinase;Inhibitor of PAS domain containing serine/threonine kinase

Item Number
P129635
Grouped product items
SKUSizeAvailabilityPrice Qty
P129635-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$64.90
P129635-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$84.90
P129635-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$169.90

Potent, selective and ATP-competitive mTOR inhibitor

Basic Description

Synonyms1H-Indol-5-ol, 2-(4-amino-1-(1-methylethyl)-1H-pyrazolo(3,4-d)pyrimidin-3-yl)- | BDBM36409 | BR164372 | UNII-H5669VNZ7V | O,N-dimethylhydroxyl-amine hydrochloride | SCHEMBL298922 | 2-[4-Amino-1-(Propan-2-Yl)-1h-Pyrazolo[3,4-D]pyrimidin-3-Yl]-1h-Indol-5-Ol
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsPP242 has been shown to be a an ATP-competitive mTORC1/mTORC2 (FRAP) inhibitor (IC50 = 8 nM). PP242 is the first selective inhibitor that targets the ATP domain of FRAP. This compound shows selectivity for FRAP over other PI 3K family kinases (IC50 values
Storage TempStore at 2-8°C
Shipped InWet ice
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of mechanistic target of rapamycin kinase;Inhibitor of PAS domain containing serine/threonine kinase
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively.
A selective FRAP inhibitor

Associated Targets(Human)

RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIP5K1C Tchem Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PRKCE Tchem Protein kinase C epsilon type (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP3K19 Tchem Mitogen-activated protein kinase kinase kinase 19 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BMPR1B Tchem Bone morphogenetic protein receptor type-1B (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BRSK1 Tchem Serine/threonine-protein kinase BRSK1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ACVR2A Tchem Activin receptor type-2A (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ACVR2B Tchem Activin receptor type-2B (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ACVR1 Tchem Activin receptor type-1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ACVRL1 Tchem Serine/threonine-protein kinase receptor R3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PASK Tchem PAS domain-containing serine/threonine-protein kinase (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK2 Tclin Tyrosine-protein kinase JAK2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MTOR Tclin Serine/threonine-protein kinase mTOR (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol
INCHI 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)
InChi Key MFAQYJIYDMLAIM-UHFFFAOYSA-N
Canonical SMILES CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N
Isomeric SMILES CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N
PubChem CID 135565635
Molecular Weight 308.34

Certificates

Certificate of Analysis(COA)

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2 results found

Lot NumberCertificate TypeDateItem
F1510068Certificate of AnalysisOct 16, 2024 P129635
L2325079Certificate of AnalysisDec 29, 2023 P129635

Chemical and Physical Properties

SolubilitySoluble in DMSO (>10 mg/mL)

Related Documents

References

1. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA.  (2008)  Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases..  Nat Chem Biol,  (11): (691-9).  [PMID:18849971] [10.1021/op500134e]
2. Zhang YM et al..  (2018)  Distant Insulin Signaling Regulates Vertebrate Pigmentation through the Sheddase Bace2..  Dev Cell,  45  (5): (580-594.e7).  [PMID:29804876]

Solution Calculators