PKC-412 (CAS 120685-11-2)
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PKC-412, a staurosporine derivative, has been shown to possess antiproliferative characteristics via inhibition of PKC (protein kinase C), Flk (kinase insert domain receptor), and c-kit. This compound has been shown to cause an increase in the G2/M phase of the cell cycle related to polyploidy, enhanced sensitivity to ionizing radiation, and apoptosis. Additionally, PKC-412 has been reported to inhibit Flt-3/Flk-2 tyrosine kinase which consequentially causes induced G1 arrest and apoptosis of Ba/F3 cell lines. Other experiments have noted that this agent demonstrates the ability to increase endothelial nitric oxide (NO) synthase expression and NO production in cultured human endothelial cells. PKC-412 is an inhibitor of c-Src, Cdk1, cyclin B, EGFR, Flk-1, Flt-1, PDGFR-β, PKA, PKC α, PKC β, PKC γ, PKC δ, PKC η, Fgr and Syk.
PKC-412 (CAS 120685-11-2) References
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- Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412. | Weisberg, E., et al. 2002. Cancer Cell. 1: 433-43. PMID: 12124173
- Patients with acute myeloid leukemia and an activating mutation in FLT3 respond to a small-molecule FLT3 tyrosine kinase inhibitor, PKC412. | Stone, RM., et al. 2005. Blood. 105: 54-60. PMID: 15345597
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- FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies. | Chen, J., et al. 2005. Oncogene. 24: 8259-67. PMID: 16091734
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- Midostaurin, enasidenib, CPX-351, gemtuzumab ozogamicin, and venetoclax bring new hope to AML. | Wei, AH. and Tiong, IS. 2017. Blood. 130: 2469-2474. PMID: 29051180
- Midostaurin reduces Regulatory T cells markers in Acute Myeloid Leukemia. | Gutierrez, L., et al. 2018. Sci Rep. 8: 17544. PMID: 30510164
- Midostaurin potentiates rituximab antitumor activity in Burkitt's lymphoma by inducing apoptosis. | Ge, X., et al. 2018. Cell Death Dis. 10: 8. PMID: 30584254
- Midostaurin Reverses ABCB1-Mediated Multidrug Resistance, an in vitro Study. | Ji, N., et al. 2019. Front Oncol. 9: 514. PMID: 31275850
- Inhibition of Bcl-2 Synergistically Enhances the Antileukemic Activity of Midostaurin and Gilteritinib in Preclinical Models of FLT3-Mutated Acute Myeloid Leukemia. | Ma, J., et al. 2019. Clin Cancer Res. 25: 6815-6826. PMID: 31320594
- Superior Efficacy of Midostaurin Over Cladribine in Advanced Systemic Mastocytosis: A Registry-Based Analysis. | Lübke, J., et al. 2022. J Clin Oncol. 40: 1783-1794. PMID: 35235417
- Combination of midostaurin and ATRA exerts dose-dependent dual effects on acute myeloid leukemia cells with wild type FLT3. | Lu, H., et al. 2022. BMC Cancer. 22: 749. PMID: 35810308
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PKC-412, 1 mg | sc-200691 | 1 mg | $51.00 | |||
PKC-412, 5 mg | sc-200691A | 5 mg | $112.00 |