PKC-412

SKU: orb1304419

Description

Midostaurin

Research Area

Cell Biology

Key Properties

• CAS Number: 120685-11-2
• MW: 570.7
• Purity: >98%
• Formula: C₃₅H₃₀N₄O₄
• SMILES: COC1C(CC2OC1(C)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13)N(C)C(=O)c1ccccc1
• Target: Kinase
• Solubility: Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 2 mg/ml).

Bioactivity

• Target IC50:
  nPKC-ε:1250 nM|c-Syk:95 nM|KDR:86 nM|APKCζ:465 μM|nPKC-δ:33 nM|Myosin light chain kinase:1900 nM|p70 S6K:5000 nM|PKCβ2:31 nM|c-Src:800 nM|c-Lyn:4300 nM|CDK1-cyclinB:570 nM|nPKC-η:160 nM|FLT1:912 nM|FLK1:3900 nM|CDK1-CyclinB:570 nM|PPK:38 nM|PKA:570 nM|EGFR:1100 nM|Protein kinase A:570 nM|c-Fgr:790 nM|PKCα:22 nM|mTOR (p70S6K):5000 nM|MLCK:1900 nM|PKCβ1:30 nM|PKCγ:24 nM|CSK:8000 nM
• 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.
• 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.
• Cell Research:
  Each well is added with 5 mM WST-1 and 0.2 mM 1-methoxy PMS and the absorbance at 450 nm is measured by a Microplate Reader.(Only for Reference)

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Midostaurin; CGP-41251

Compound Identifiers

PubChem CID

16760627