Replaces Prod. #: ALX-380-281
Inhibitor of a variety of serine/threonine and tyrosine kinases, like protein kinase C (PKC), cyclic AMP-dependent protein kinase (PKA), S6 kinase, Akt (protein kinase B; PKB), epidermal growth factor receptor (EGFR) tyrosine kinase activity and others including KDR, VEGFR, PDGFR, c-kit and other receptor tyrosine kinases. Potently inhibits FLT-3 kinase including mutant forms found in acute myeloid leukemia in vitro and in vivo. Apoptosis inducer. Showed broad antiproliferative activity against various tumor cell lines. Selectively inhibits T lymphocyte production of TNF-α. Upregulates endothelial nitric oxide synthase (eNOS; NOS III). Abrogates tumor angiogenesis in vivo.
Product Details
| Alternative Name: | 4'-N-Benzoyl-staurosporine, Midostaurin, CGP 41251 |
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| Formula: | C35H30N4O4 |
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| MW: | 570.6 |
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| CAS: | 120685-11-2 |
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| MI: | 14: 6185 |
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| Purity: | ≥98% (TLC) |
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| Appearance: | White to off-white powder. |
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| Solubility: | Soluble in DMSO (15mg/ml), MDC (10mg/ml), methanol (5mg/ml) or 100% ethanol (2.5mg/ml). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for up to 1 year after receipt when stored at -20°C. Stock solutions are stable for up to 3 months at -20°C. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
The FLT3 inhibitor PKC412 exerts differential cell cycle effects on leukemic cells depending on the presence of FLT3 mutations: T. Odgerel, et al.; Oncogene
27, 3102 (2008),
Abstract;
The FLT3 inhibitor PKC412 in combination with cytostatic drugs in vitro in acute myeloid leukemia: L. Möllgard, et al.; Cancer Chemother. Pharmacol.
62, 439 (2008),
Abstract;
Divergent cytotoxic effects of PKC412 in combination with conventional antileukemic agents in FLT3 mutation-positive versus -negative leukemia cell lines: Y. Furukawa, et al.; Leukemia
21, 1005 (2007),
Abstract;
PKC 412 small-molecule tyrosine kinase inhibitor: single-compound therapy for pancreatic cancer: J. El Fitori, et al.; Cancer
110, 1457 (2007),
Abstract;
PKC412 (CGP41251) modulates the proliferation and lipopolysaccharide-induced inflammatory responses of RAW 264.7 macrophages: K. Miyatake, et al.; BBRC
360, 115 (2007),
Abstract;
PKC412 demonstrates JNK-dependent activity against human multiple myeloma cells: J. Sharkey, et al.; Blood
109, 1712 (2007),
Abstract;
Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT: K.V. Gleixner, et al.; Haematologica
92, 1451 (2007),
Abstract;
Full Text
Antitumor and normal cell protective effect of PKC412 in the athymic mouse model of ovarian cancer: M. Kim, et al.; Ann. Clin. Lab. Sci.
36, 455 (2006),
Abstract;
Inhibitors of the PI3-kinase/Akt pathway induce mitotic catastrophe in non-small cell lung cancer cells: T.H. Hemström, et al.; Int. J. Cancer
119, 1028 (2006),
Abstract;
PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects: K.V. Gleixner, et al.; Blood
107, 752 (2006),
Abstract;
Full Text
Effects of the kinase inhibitor CGP41251 (PKC 412) on lymphocyte activation and TNF-alpha production: M.S. Si, et al.; Int. Immunopharmacol.
5, 1141 (2005),
Abstract;
FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies: J. Chen, et al.; Oncogene
24, 8259 (2005),
Abstract;
Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouse: H. Li, et al.; Nitric Oxide
12, 231 (2005),
Abstract;
N-Benzoylstaurosporine (PKC412) inhibits Akt kinase inducing apoptosis in multiple myeloma cells: N.J. Bahlis, et al.; Leuk. Lymphoma
46, 899 (2005),
Abstract;
Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412: R.M. Stone, et al.; Blood
105, 54 (2005),
Abstract;
Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3: P. George, et al.; Cancer Res.
64, 3645 (2004),
Abstract;
Full Text
PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder: J. Chen, et al.; PNAS
101, 14479 (2004),
Abstract;
Full Text
A protein kinase C inhibitor induces phenotypic reversion of ras-transformed pancreatic cancer cells and cooperatively blocks tumor cell proliferation with an anti- ras peptide.: D. Way, et al.; Cancer Chemother. Pharmacol.
49, 429 (2002),
Abstract;
Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412: E. Weisberg, et al.; Cancer Cell
1, 433 (2002),
Abstract;
Protein kinase C inhibitors: H.C. Swannie & S.B. Kaye; Curr. Oncol. Rep.
4, 37 (2002), (Review),
Abstract;
Phase I and pharmacokinetic study of PKC412, an inhibitor of protein kinase C: D.J. Propper, et al.; J. Clin. Oncol.
19, 1485 (2001),
Abstract;
Full Text
The phosphatidylinositide 3’-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C: A. Tenzer, et al.; Cancer Res.
61, 8203 (2001),
Abstract;
Full Text
PKC412--a protein kinase inhibitor with a broad therapeutic potential: D. Fabbro, et al.; Anticancer Drug Des.
15, 17 (2000),
Abstract;
Differential effects of UCN-01, staurosporine and CGP 41 251 on cell cycle progression and CDC2/cyclin B1 regulation in A431 cells synchronized at M phase by nocodazole: T. Akiyama, et al.; Anticancer Drugs
10, 67 (1999),
Abstract;
Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent: D. Fabbro, et al.; Pharmacol. Ther.
82, 293 (1999),
Abstract;
Analogs of staurosporine: potential anticancer drugs?: A. Gescher; Gen. Pharmacol.
31, 721 (1998), (Review),
Abstract;
Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251: E. Andrejauskas-Buchdunger & U. Regenass; Cancer Res.
52, 5353 (1992),
Abstract;
Full Text
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