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Midostaurin

Cat. No. M2850
Midostaurin  Structure
Synonym:

PKC412

Size Price Availability Quantity
1mg USD 50  USD50 In stock
5mg USD 100  USD100 In stock
10mg USD 160  USD160 In stock
50mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

Midostaurin (pkc412) is a multi-targeted kinase inhibitor, including PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 80-500 nM. PKC412 showed a broad antiproliferative activity against various tumor and normal cell lines in vitro, and was able to reverse the Pgp-mediated multidrug resistance of tumor cells in vitro. PKC412 displayed a potent antitumor activity as single agent and was able to potentiate the antitumor activity of some of the clinically used cytotoxins (Taxol and doxorubicin) in vivo. Orally administered PKC412 also strongly inhibited retinal neovascularization as well as laser-induced choroidal neovascularization in murine models.

Product Citations
Chemical Information
Molecular Weight 570.64
Formula C35H30N4O4
CAS Number 120685-11-2
Solubility (25°C) DMSO 29 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Laura K Schmalbrock, et al. Clonal evolution of acute myeloid leukemia with FLT3-ITD mutation under treatment with midostaurin

[2] Jannik Stemler, et al. Antifungal prophylaxis and novel drugs in acute myeloid leukemia: the midostaurin and posaconazole dilemma

[3] No authors listed. Midostaurin

[4] No authors listed. Midostaurin

[5] Richard M Stone, et al. Midostaurin plus Chemotherapy for Acute Myeloid Leukemia with a FLT3 Mutation

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Keywords: Midostaurin , PKC412 supplier, PKC, inhibitors, activators


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