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PKC412

Chemical Structure : PKC412

CAS No.: 120685-11-2

PKC412 (CGP-41231;CGP-41251;Midostaurin;PKC-412;CGP41231;CGP41251)

Catalog No.: PC-42473Not For Human Use, Lab Use Only.

Midostaurin (CGP41231, PKC-412) is a potent, selective PKC inhibitor with IC50 of 50 nM, also inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 of 20-500 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Midostaurin (CGP41231, PKC-412) is a potent, selective PKC inhibitor with IC50 of 50 nM, also inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 of 20-500 nM. 
Midostaurin (CGP41231, PKC-412) 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.
Midostaurin (CGP41231, PKC-412) inhibits human brain tumors cells (mean IC50=0.4 uM), displays antitumor activity in vivo.

Physicochemical Properties

M.Wt 570.6371
Formula C35H30N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 21 mg/mL

Chemical Name/SMILES

Benzamide, 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-

References

1. Meyer T, et al. Int J Cancer. 1989 May 15;43(5):851-6.

2. Krause KH, et al. Eur J Pharmacol. 1992 Oct 1;227(2):221-4.

3. Amon U, et al. Pharmacology. 1993 Sep;47(3):200-8.

4. Begemann M, et al. Clin Cancer Res. 1996 Jun;2(6):1017-30.

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