PKC412

Name: PKC412
SKU: P4008
Availability: InStock

Product ID P4008

Cas No. 120685-11-2

Purity ≥98%

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Description

PKC412 is an anti-metastatic and anticancer chemotherapeutic staurosporine derivative that inhibits FMS-like tyrosine kinase 3 (FLT3) and is currently in clinical trials as a potential treatment for acute myelogenous leukemia (AML). PKC412 also inhibits PKC. In keloid-derived fibroblasts, PKC412 increases activity of caspase 3, inducing apoptosis. In animal models of melanoma, PKC412 inhibits metastasis and platelet-aggregating activity. This compound also alters differentiation patterns of dendritic cells ex vivo.

Product Info

Cas No.	120685-11-2
Purity	≥98%
Formula	C₃₅H₃₀N₄O₄
Formula Wt.	570.64
IUPAC Name	N-[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-N-methylbenzamide
Synonym	Midostaurin, 4'-N-Benzoyl staurosporine
Melting Point	235-260°C
Solubility	DMSO, Dichloromethanol
Appearance	Off white powder

Shipping and Storage

Store Temp	4°C
Ship Temp	Ambient

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MSDS	P4008 MSDS PDF
Info Sheet	P4008 Info Sheet PDF

References

Fischer T, Stone RM, Deangelo DJ, et al. Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3. J Clin Oncol. 2010 Oct 1;28(28):4339-45. PMID: 20733134.

Huang YC, Shieh HR, Chen YJ. Midostaurin (PKC412) modulates differentiation and maturation of human myeloid dendritic cells. Toxicol In Vitro. 2010 Sep;24(6):1705-10. PMID: 20685248.

Stölzel F, Steudel C, Oelschlägel U, et al. Mechanisms of resistance against PKC412 in resistant FLT3-ITD positive human acute myeloid leukemia cells. Ann Hematol. 2010 Jul;89(7):653-62. PMID: 20119833.

Nakazono-Kusaba A, Takahashi-Yanaga F, Miwa Y, et al. PKC412 induces apoptosis through a caspase-dependent mechanism in human keloid-derived fibroblasts. Eur J Pharmacol. 2004 Aug 23;497(2):155-60. PMID: 15306200.

Yoshikawa N, Nakamura K, Yamaguchi Y, et al. Effect of PKC412, a selective inhibitor of protein kinase C, on lung metastasis in mice injected with B16 melanoma cells. Life Sci. 2003 Feb 7;72(12):1377-87. PMID: 12527035.

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PKC412

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