PKC412(midostaurin) Inhibitor CAS No. 120685-11-2

Product Name	PKC412(midostaurin)
CAS No.	120685-11-2
Molecular Weight	570.64
Formula	C₃₅H₃₀N₄O₄
Chemical Name	(9S,10R,11R,13R)-2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-11-(methylamino)-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiamzonine-1-one
Smiles	C(=O)(c1ccccc1)N(C)C1C[C@H]2n3c4c5n(c6c(c5c5c(c4c4c3cccc4)C(=O)NC5)cccc6)[C@@]([C@H]1OC)(O2)C
Chemical Structure

Biological activities

PKC412 is a selective protein kinase C (PKC) inhibitor. PKC412 shows antitumor activity in vitro and in vivo. PKC412 preferentially inhibits the conventional PKC subtype such as cPKC-α, cPKC-β1, cPKC-β2, cPKC-γ, nPKC-δ and nPKC-η with IC50s of 0.022, 0.03, 0.031, 0.024, 0.33, 0.16µM, respectively. In an in vitro test, PKC412 causes significant inhibition of cell proliferation for 24-48 hours in A549 and NCI-H520 cells at the concentration of 0.5 and 1.0 µM respectively.^[1] PKC412 increases in the G2/M phase of cell cycle accompanying with increased polyploidy, apoptosis and enhanced sensitivity to ionizing radiation in a dose-dependent manner.^[2] PKC412 inhibits autophosphorylation of the receptors such as platelet-derived growth factor (PDGF), stem cell factor (SCF), and kinase insert domain-containing receptor (KDR)^[3] In vivo, PKC412 inhibits the tumor growth at the dose of 200mg/kg in nude mice that are transplanted with A549 and NCI-H520 cells, and the T/C values against A549 and NCI-H520 are 38.6% and 34.3%, respectively. It also shows that PKC412 reduces the particulate PKC activity but not the cytosolic PKC activity.^[1]

Protocols

PKC412 is dissolved in DMSO in vitro tests. In vivo tests, PKC412 is added to sterile water and then sonicated for 10 min to be a milky suspension before use.^[1]

References

[1] Ikegami Y, Yano S, Nakao K. Antitumor effect of CGP41251, a new selective protein kinase C inhibitor, on human non-small cell lung cancer cells. Jpn J Pharmacol. 1996, 70 (1):65-72. [2] Fabbro D, Ruetz S, Bodis S, Pruschy M, Csermak K, Man A, Campochiaro P, Wood J, O'Reilly T, Meyer T. PKC412--a protein kinase inhibitor with a broad therapeutic potential. Anticancer Drug Des. 2000, 15 (1):17-28. [3] Fabbro D, et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent. Pharmacol Ther. 1999, 82(2-3): 293-301.

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