PKC 412 (Midostaurin)

Catalog No. A12650

PKC 412 (Midostaurin)是一种广谱蛋白激酶抑制剂。抑制常规PKC亚型α/β/γ，PDFRβ，VEGFR2，Syk，Flk-1，Flt3，Cdk1/B，PKA，c-Kit，c-Fgr，c-Src，VEGFR1和EGFR。显示有效的抗肿瘤活性。

Technical details

Catalog Num	A12650
M. Wt	570.64
Formula	C35H30N4O4
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	120685-11-2
Synonyms	CGP 41251, PKC412, PKC-412, CGP41251, CGP-41251
SMILES	C[C@@]12[C@@H]([C@@H](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)N(C)C(=O)C9=CC=CC=C9)OC

Biological Activity

Targets

Target	Value
PKCα	IC50: 22nM
PKCγ	IC50: 24nM
PKCβ1	IC50: 30nM
PKCβ2	IC50: 31nM
PPK	IC50: 38nM
KDR	IC50: 86nM
c-Syk	IC50: 95nM
PKCη	IC50: 160nM
PKCδ	IC50: 330nM
Flk1	IC50: 390nM
CDK1/CyclinB	IC50: 570nM
PKA	IC50: 570nM
c-FGR	IC50: 790nM
c-Src	IC50: 800nM
FLT1	IC50: 912nM
PLK1	IC50: >1.0μM
p38	IC50: >1μM
Tie-1	IC50: >1μM
c-Met	IC50: >1μM
EGFR	IC50: 1.1μM
PKCε	IC50: 1.25μM
Myosin-lightchainkinase	IC50: 1.9μM
c-Lyn	IC50: 4.30μM
p70S6K	IC50: 5.0μM
CSK	IC50: 8.0μM
CDK4/CyclinD1	IC50: >10μM
Junkinase	IC50: >10μM
Tie-2	IC50: >10μM
FGFR1	IC50: >10μM
v-Abl	IC50: >100μM
ERK1	IC50: >200μM
CK1	IC50: >200μM
CK2	IC50: >200μM
PKB	IC50: >300μM
PKCζ	IC50: 465μM

Solubility *

In vitro (25°C)	DMSO	90 mg/mL (157.72 mM)
	Water	Insoluble
	Ethanol	Warmed: 18 mg/mL
In vivo	5% DMSO+45% PEG 300+ddH2O	3 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	17.52 mL	87.62 mL	175.24 mL
0.5 mM	3.5 mL	17.52 mL	35.05 mL
1 mM	1.75 mL	8.76 mL	17.52 mL
5 mM	0.35 mL	1.75 mL	3.5 mL

*The above data is based on the productmolecular weight 570.64. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.