Antibodies
Midostaurin (PKC412)
- 貨號 Cat. No.
- S8064
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Midostaurin (PKC412)
Catalog No.S8064
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 andVEGFR1/2 with IC50 ranging from 80-500 nM.
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Biological Activity
| Description | 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. | |||||
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| Targets | PKCα | PKCβ | PKCγ | c-Syk | KDR | |
| IC50 | 22 nM | 30 nM | 24 nM | 95 nM | 82 nM [1] | |
| 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. [1] | |||||
| 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. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
Cell Assay: [2]
| Cell lines | A549, NCI-H520 |
|---|---|
| Concentrations | ~1.0 μM |
| Incubation Time | 24-72 h |
| Method | 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. |
Animal Study: [1]
| Animal Models | Colo 205 colorectal tumors xenograft |
|---|---|
| Dosages | 50 mg/kg, 200 mg/kg, once daily |
| Administration | p.o. |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01282502 | Recruiting | Adenocarcinoma of the Rectum | Massachusetts General Hospital | 2011-08 | Phase 1 |
| NCT01830361 | Recruiting | Acute Myeloid Leukemia | Dresden University of Technology|Novartis Pharmaceuticals | 2012-04 | Phase 2 |
| NCT01477606 | Recruiting | Acute Myeloid Leukemia | University of Ulm|Novartis Pharmaceuticals | 2012-05 | Phase 2 |
| NCT01846624 | Recruiting | Acute Myeloid Leukemia With Multilineage Dysplasia Following Myelodysplastic Syndrome|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q) etc. | Stanford University|Bruno C. Medeiros|National Cancer Institute (NCI) | 2013-06 | Phase 2 |
| NCT01883362 | Not yet recruiting | Acute Myeloid Leukemia | Novartis|Novartis Pharmaceuticals | 2013-09 | Phase 2 |
Chemical Information
Download Midostaurin (PKC412) SDF
| Molecular Weight (MW) | 570.64 |
|---|---|
| Formula | C35H30N4O4 |
| CAS No. | 120685-11-2 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | CGP 41251 |
| Solubility (25°C) * | In vitro | DMSO | mg/mL (<1 mM) |
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| Water | mg/mL (<1 mM) | ||
| Ethanol | mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck 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. | |||
| Chemical Name | 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- |
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