Midostaurin, also known as PKC-412, PKC-412A and CGP 41251; is a synthetic indolocarbazole multikinase inhibitor with potential antiangiogenic and antineoplastic activities. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors. Midostaurin was approved in 2017.
Chemical Formula: C35H30N4O4
Exact Mass: 570.22671
Molecular Weight: 570.6371
Elemental Analysis: C, 73.67; H, 5.30; N, 9.82; O, 11.22
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not soluble in water.
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
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.
- Wang ES. Beyond midostaurin: Which are the most promising FLT3 inhibitors in AML? Best Pract Res Clin Haematol. 2019 Dec;32(4):101103. doi: 10.1016/j.beha.2019.101103. Epub 2019 Oct 18. Review. PubMed PMID: 31779982.
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- Midostaurin for acute myeloid leukaemia, mastocytosis, and mast cell leukaemia. Aust Prescr. 2019 Apr;42(2):73-74. doi: 10.18773/austprescr.2019.017. Epub 2019 Feb 28. Review. PubMed PMID: 31048943; PubMed Central PMCID: PMC6478956.
- Sly N, Gaspar K. Midostaurin for the management of FLT3-mutated acute myeloid leukemia and advanced systemic mastocytosis. Am J Health Syst Pharm. 2019 Feb 9;76(5):268-274. doi: 10.1093/ajhp/zxy050. Review. PubMed PMID: 30753289.
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