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INK 128 (MLN0128) - ≥98%, high purity , Serine/threonine-protein kinase mTOR inhibitor, CAS No.1224844-38-5, Serine/threonine-protein kinase mTOR inhibitor

  • Moligand™
  • ≥98%
Item Number
I128086
Grouped product items
SKUSizeAvailabilityPrice Qty
I128086-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$94.90
I128086-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$427.90
I128086-100mg
100mg
In stock
$533.90

Basic Description

SynonymsSapanisertib|1224844-38-5|INK-128|MLN0128|INK 128|INK128|TAK-228|MLN-0128|5-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)benzo[d]oxazol-2-amine|INK 128 (MLN0128)|Sapanisertib (MLN0128)|UNII-JGH0DF1U03|JGH0DF1U03|CB-228|3-(2-Amino-5-benzoxazolyl)-
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsINK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases [1]. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inh
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionSerine/threonine-protein kinase mTOR inhibitor
Note5mg卖完停产,不再备货
Product Description

INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin).
A potent and selective TORC1/2 inhibitor

Product Properties

ALogP1.7

Associated Targets

RPTOR Tbio Regulatory-associated protein of mTOR 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPKAP1 Tbio Target of rapamycin complex 2 subunit MAPKAP1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

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 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIK3CB Tchem Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 0 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)

PI4KB Tchem Phosphatidylinositol 4-kinase beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIK3C3 Tchem Phosphatidylinositol 3-kinase catalytic subunit type 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RPS6KB1 Tchem Ribosomal protein S6 kinase beta-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MTOR Tclin Serine/threonine-protein kinase mTOR 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine
INCHI InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19)
InChi Key GYLDXIAOMVERTK-UHFFFAOYSA-N
Canonical SMILES CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N
Isomeric SMILES CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N
PubChem CID 45375953
Molecular Weight 309.33

Certificates

Certificate of Analysis(COA)

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2 results found

Lot NumberCertificate TypeDateItem
B2225533Certificate of AnalysisDec 14, 2023 I128086
E1705099Certificate of AnalysisDec 08, 2022 I128086

Chemical and Physical Properties

SolubilityDMSO

Related Documents

References

1. Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS.  (2009)  mTOR Mediated Anti-Cancer Drug Discovery..  Drug Discov Today Ther Strateg,  (2): (47-55).  [PMID:20622997]
2. Schenone S, Brullo C, Musumeci F, Radi M, Botta M.  (2011)  ATP-competitive inhibitors of mTOR: an update..  Curr Med Chem,  18  (20): (2995-3014).  [PMID:21651476]
3. Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, Shi EY, Stumpf CR, Christensen C, Bonham MJ et al..  (2012)  The translational landscape of mTOR signalling steers cancer initiation and metastasis..  Nature,  485  (7396): (55-61).  [PMID:22367541]
4. Arendse LB, Murithi JM, Qahash T, Pasaje CFA, Godoy LC, Dey S, Gibhard L, Ghidelli-Disse S, Drewes G, Bantscheff M et al..  (2022)  The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages..  Sci Transl Med,  14  (667): (eabo7219).  [PMID:36260689]

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