Kinase inhibitor with potential use in cancer treatment
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PKC 412

Item No. 10459

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methyl-benzamide
CAS Number
120685-11-2
Synonyms
  • N-Benzoylstaurosporine
  • CGP 41231
  • CGP 41251
  • Midostaurin
Molecular Formula
C35H30N4O4
Formula Weight
570.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 14 mg/ml
λmax
244, 293, 334, 355, 372 nm
SMILES
O=C1NCC2=C3C(N4C5=C3C=CC=C5)=C6C(C(C=CC=C7)=C7N6[C@@]8([H])C[C@@H](N(C(C9=CC=CC=C9)=O)C)[C@@H](OC)[C@]4(C)O8)=C21
InChi Code
InChI=1S/C35H30N4O4/c1-35-32(42-3)25(37(2)34(41)19-11-5-4-6-12-19)17-26(43-35)38-23-15-9-7-13-20(23)28-29-22(18-36-33(29)40)27-21-14-8-10-16-24(21)39(35)31(27)30(28)38/h4-16,25-26,32H,17-18H2,1-3H3,(H,36,40)/t25-,26-,32-,35+/m1/s1
InChi Key
BMGQWWVMWDBQGC-IIFHNQTCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $31

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    5 mg

    $93

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    10 mg

    $154

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    25 mg

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    Product Description

    PKC 412 is a cell-permeable, reversible inhibitor of several serine/threonine and tyrosine kinases, including conventional PKC isoforms (α, β, and γ), Syk, FLK1, Akt, PKA, c-Kit, C-Fgr, c-Src, FLT3, PDFRβ, VEGFR1, and VEGFR2 with IC50 values ranging from 80-500 nM.1,2,3,4 It also upregulates the expression of endothelial nitric oxide synthase (eNOS) in mice.5 PKC 412 inhibits growth or induces apoptosis in many cancer cell types, blocks angiogenesis in tumors, and sensitizes cancer cells to ionizing radiation, supporting its use in cancer therapy.1,6,7

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fabbro, D., Buchdunger, E., Wood, J., et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent. Pharmacol. Ther. 82(2-3), 293-301 (1999).

    2. Ozaki, H., Seo, M.S., Ozaki, K., et al. Blockade of vascular endothelial cell growth factor receptor signaling is sufficient to completely prevent retinal neovascularization. Am. J. Pathol. 156(2), 697-707 (2000).

    3. Tenzer, A., Zingg, D., Rocha, S., et al. The phosphatidylinositide 3'-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C. Cancer Res. 61(22), 8203-8210 (2001).

    4. Andrejauskas-Buchdunger, E., and Regenass, U. Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251. Cancer Res. 52(19), 5353-5358 (1992).

    5. Li, H., Hergert, S.M., Schäfer, S.C., et al. Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouse. Nitric Oxide 12(4), 231-236 (2005).

    6. Marmy-Conus, N., Hannan, K.M., and Pearson, R.B. Ro 31-6045, the inactive analogue of the protein kinase C inhibitor Ro 31-8220, blocks in vivo activation of p70s6k/p85s6k: Implications for the analysis of S6K signalling. FEBS Lett. 519(1-3), 135-140 (2002).

    7. El Fitori, J., Su, Y., Büchler, P., et al. PKC412 small-molecule tyrosine kinase inhibitor: Single-compound therapy for pancreatic cancer. Cancer 110(7), 1457-1468 (2007).