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CH5132799 - ≥97%, high purity , PI3-kinase class I inhibitor, CAS No.1007207-67-1, PI3-kinase class I inhibitor

Item Number
C127596
Grouped product items
SKUSizeAvailabilityPrice Qty
C127596-1mg
1mg
In stock
$56.90
C127596-5mg
5mg
In stock
$234.90
C127596-10mg
10mg
In stock
$365.90
C127596-25mg
25mg
In stock
$823.90
C127596-50mg
50mg
In stock
$1,018.90
C127596-100mg
100mg
In stock
$1,436.90

Basic Description

SynonymsUNII-JCL936W835 | AC-28422 | 5-(7-methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine | JCL936W835 | HMS3656H15 | SCHEMBL2377154 | Q27075949 | 5-[7-(methylsulfonyl)-2-(morpholin-4-yl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyri
Specifications & PurityMoligand™, ≥97%
Biochemical and Physiological MechanismsCH5132799 selectively inhibits class I PI3Ks, such as PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ with IC50 values of 0.014, 0.12, 05.0, and 0.36 μM, respectively. CH5132799 shows less inhibition of class II PI3Ks, class III PI3ks, and mTOR. CH5132799 suppresses phosp
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionPI3-kinase class I inhibitor
Product Description

CH5132799 inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines.
A PI3K and FRAP inhibitor

Product Properties

ALogP-0.6

Associated Targets(Human)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIK3CB Tchem Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIK3CD Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MTOR Tclin Serine/threonine-protein kinase mTOR (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PIK3CD Tclin PI3-kinase p110-delta subunit (6699 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PIK3CG Tclin PI3-kinase p110-gamma subunit (5411 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PIK3CB Tchem PI3-kinase p110-beta subunit (4044 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PC-3 (62116 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SK-OV-3 (52876 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
T47D (39041 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HCT-116 (91556 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PIK3C2B Tchem Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide (438 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver microsomes (16955 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PIK3C3 Tchem Phosphatidylinositol 3-kinase catalytic subunit type 3 (535 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PIK3C2A Tchem Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha (139 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ME-180 (202 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MFE-280 (151 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

PIK3CA PI3-kinase p110-alpha subunit (51 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rhesus monkey (3147 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences
PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

FDA: [1]


PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

Other: [1]


PubMed: [1]


PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

PubMed: [1]


PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

PubMed: [1] , [2]


PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

Other: [1]


PubMed: [1]


PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

DOI: [1]


Other: [1]


PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

Other: [1]


PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

Other: [1]


PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

PubMed: [1]


PI3-kinase p110-delta subunit inhibitorINHIBITORALA3130PI3-kinase p110-delta subunitSINGLE PROTEINHomo sapiens

PubMed: [1]


Names and Identifiers

Pubchem Sid488201430
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488201430
IUPAC Name 5-(7-methylsulfonyl-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine
INCHI InChI=1S/C15H19N7O3S/c1-26(23,24)22-3-2-11-12(10-8-17-14(16)18-9-10)19-15(20-13(11)22)21-4-6-25-7-5-21/h8-9H,2-7H2,1H3,(H2,16,17,18)
InChi Key JEGHXKRHKHPBJD-UHFFFAOYSA-N
Canonical SMILES CS(=O)(=O)N1CCC2=C(N=C(N=C21)N3CCOCC3)C4=CN=C(N=C4)N
Isomeric SMILES CS(=O)(=O)N1CCC2=C(N=C(N=C21)N3CCOCC3)C4=CN=C(N=C4)N
PubChem CID 49784945
Molecular Weight 377.42

Certificates

Certificate of Analysis(COA)

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12 results found

Lot NumberCertificate TypeDateItem
C23231058Certificate of AnalysisJan 16, 2023 C127596
C23231059Certificate of AnalysisJan 16, 2023 C127596
C23231060Certificate of AnalysisJan 16, 2023 C127596
C23231061Certificate of AnalysisJan 16, 2023 C127596
C2323350Certificate of AnalysisJan 16, 2023 C127596
C2323359Certificate of AnalysisJan 16, 2023 C127596
C2323360Certificate of AnalysisJan 16, 2023 C127596
C2323387Certificate of AnalysisJan 16, 2023 C127596
C2323603Certificate of AnalysisJan 16, 2023 C127596
C2323620Certificate of AnalysisJan 16, 2023 C127596
C2323691Certificate of AnalysisJan 16, 2023 C127596
C2323738Certificate of AnalysisJan 16, 2023 C127596

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Chemical and Physical Properties

SolubilityDMSO 12 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

Related Documents

References

1. Ohwada J, Ebiike H, Kawada H, Tsukazaki M, Nakamura M, Miyazaki T, Morikami K, Yoshinari K, Yoshida M, Kondoh O et al..  (2011)  Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799..  Bioorg Med Chem Lett,  21  (6): (1767-72).  [PMID:21316229] [10.1021/op500134e]

Solution Calculators