PKC412

SKU: orb1226798

Description

A potent, selective PKC inhibitor with IC50 of 50 nM; displays a high degree of selectivity over PKA (IC50=2.4 uM), S6 kinase (IC50=5.0 uM) and EGFR (IC50=3.0 uM) compared with Staurosporine; inhibits human brain tumors cells (mean IC50=0.4 uM), displays antitumor activity in vivo.Blood Cancer Phase 3 Clinical(In Vitro):Midostaurin (PKC412) shows a broad antiproliferative activity against various tumor and normal cell lines in vitro, and is able to reverse the Pgp-mediated multidrug resistance of tumor cells in vitro. Exposure of cells to Midostaurin (PKC412) results in a dose-dependent increase in the G2/M phase of the cell cycle concomitant with increased polyploidy, apoptosis and enhanced sensitivity to ionizing radiation. Midostaurin (PKC412) induces substantial inhibition of KIT-, Lyn-, and STAT5 activity, but does not suppress Btk in HMC-1 cells and primary neoplastic mast cells. Midostaurin (PKC412) inhibits EN fusion tyrosine kinase in hematopoietic Ba/F3 cells. Midostaurin (PKC412) significantly inhibits EN phosphorylation in M0-91 and IMS-M2 cells in a dose-dependent manner.(In Vivo):Midostaurin (PKC412) strongly inhibits retinal neovascularization as well as laser-induced choroidal neovascularization in murine models. Midostaurin (PKC412) (25 mg/kg, i.p.) protects mouse livers of the K18 Arg90Cys-overexpressing transgenic mice from Fas-induced apoptosis.

Key Properties

• CAS Number: 120685-11-2
• MW: 570.6371
• Purity: >98% (HPLC)
• Formula: C₃₅H₃₀N₄O₄
• SMILES: C[C@@]12[C@H](OC)[C@H](N(C(C3=CC=CC=C3)=O)C)C[C@H](N4C5=CC=CC=C5C6=C7C(CNC7=O)=C8C9=CC=CC=C9N2C8=C64)O1
• Target: PKC
• Solubility: DMSO: ≥ 21 mg/mL

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CGP-41231 | CGP-41251 | Midostaurin | PKC-412

Quick Database Links

Gene Symbol

PKC