[CAS NO. 120685-11-2] Midostaurin (PKC412)

Name: Midostaurin (PKC412)
Brand: Arctom Scientific
SKU: SLK-S8064

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [120685-11-2]

Store

Catalog

SLK-S8064

Brand

Selleck

CAS

120685-11-2

DESCRIPTION [120685-11-2]

Overview

MDL	MFCD00871372
Molecular Weight	570.64
Molecular Formula	C35H30N4O4
SMILES	C[C@]12N3C=4C5=C(C6=C(C4C=7C3=CC=CC7)CNC6=O)C=8C(N5[C@@H](O1)C[C@@H](N(C(=O)C9=CC=CC=C9)C)[C@H]2OC)=CC=CC8

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.7524 mL	8.7621 mL	17.5242 mL
5 mM	0.3505 mL	1.7524 mL	3.5048 mL
10 mM	0.1752 mL	0.8762 mL	1.7524 mL
50 mM	0.0350 mL	0.1752 mL	0.3505 mL

Description

Midostaurin (pkc412, CGP 41251) is a multi-targeted kinase inhibitor, including , , , , , , , , , and with ranging from 80-500 nM.

Targets

In vitro

Midostaurin(pkc412) is a broad spectrum protein kinase inhibitor. Midostaurin(pkc412) interacts strongly with ATP binding sites of the conventional PKC-α, -β and -γ, PDGFRβ, VEGF-R2, VEGF-R1 and the cyclin-dependant kinase 1-cyclin B complex. Midostaurin(pkc412) inhibits the growth of various human and animal cell lines in vitro at similar submicromolar concentrations. Midostaurin(pkc412) also effectively inhibits the in vitro proliferation of glioblastoma and induced the accumulation of cells in G2/M and formation of giant nuclei with extensive fragmentation and apoptotic bodies. Midostaurin(pkc412) is able to reverse the p-glycoprotein-mediated multidrug resistance of tumor cells in vitro.

In vivo

Midostaurin(pkc412) may suppress tumor growth by inhibiting tumor angiogenesis (via its effects on the VEGF receptor tyrosine kinases) in addition to directly inhibiting tumor cell proliferation (via its effects on PKCs). This anti-angiogenic action may contribute to the antimetastatic and broad antitumor activity displayed by midostaurin(pkc412), as well as the synergy with cytotoxic agents, including doxorubicin, cyclophosphamide, cisplatin and gemcitabine. When given orally, the maximally tolerated dose for midostaurin(pkc412) is >300 mg/kg.

References

[1] Fabbro D, et al. Pharmacol Ther, 1999, 82(2-3), 293-301.
[2] Ikegami Y, et al. Jpn J Pharmacol, 1996, 70(1), 65-72.

Synonyms

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-

Benzamide, N-(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-, [9S-(9α,10β,11β,13α)]-

9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3′,2′,1′-lm]pyrrolo[3,4-j][1,7]benzodiazonine, benzamide deriv.

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-methylbenzamide

CGP 41251

Benzoylstaurosporine

N-Benzoylstaurosporine

CGP 41231

Midostaurin

PKC 412

Rydapt