Inhibitor of TORC1/2
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INK128

Item No. 11811

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(2-amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
CAS Number
1224844-38-5
Synonyms
  • MLN0128
Molecular Formula
C15H15N7O
Formula Weight
309.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 2 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
205, 243, 292 nm
SMILES
CC(C)N1C2=NC=NC(N)=C2C(C3=CC(N=C(N)O4)=C4C=C3)=N1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

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    10 mg

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    50 mg

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    Product Description

    INK128 is an inhibitor of TORC1/2, acting as an ATP-dependent inhibitor of mTOR kinase (IC50 = 1 nM).1,2,3 It blocks the phosphorylation of downstream substrates of both TORC1 and TORC2.2 INK128 interferes with the growth of cell lines which are resistant to rapamycin and pan-PI3K inhibitors.2,4 Moreover, daily, oral administration of INK128 inhibits angiogenesis and tumor growth in several xenograft models.2 The effects of INK128 on gene expression also reduce invasion and metastasis.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liu, Q., Thoreen, C., Wang, J., et al. mTOR mediated anti-cancer drug discovery. Drug Discov. Today Ther. Strateg. 6(2), 47-55 (2009).

    2. Jessen, K., Wang, S., Kessler, L., et al. Abstract B148: INK128 is a potent and selective TORC1/2 inhibitor with broad oral antitumor activity. Mol. Cancer Ther. 8(12), B148 (2009).

    3. Schenone, S., Brullo, C., Musumeci, F., et al. ATP-competitive inhibitors of mTOR: An update. Curr. Med. Chem. 18(20), 2995-3014 (2011).

    4. Maiso, P., Liu, Y., Morgan, B., et al. Defining the role of TORC1/2 in multiple myeloma. Blood 118(26), 6860-6870 (2011).

    5. Hsieh, A.C., Liu, Y., Edlind, M.P., et al. The translational landscape of mTOR signalling steers cancer initiation and metastasis. Nature 485(7396), 55-61 (2012).