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PKC-412

Flt inhibitor
 
BML-EI370-0001 1 mg 122.00 USD
 
BML-EI370-0005 5 mg 483.00 USD
Do you need bulk/larger quantities?
 
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 Specification

Alternative Name:4'-N-Benzoyl-staurosporine, Midostaurin, CGP 41251
 
Formula:C35H30N4O4
 
MW:570.6
 
CAS:120685-11-2
 
MI:14: 6185
 
Purity:≥98% (TLC)
 
Appearance:White to off-white powder.
 
Solubility:Soluble in DMSO (15mg/ml), MDC (10mg/ml), methanol (5mg/ml) or 100% ethanol (2.5mg/ml).
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
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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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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