PKC-412 (CAS 120685-11-2)

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Alternate Names: Midostaurin; 4'-N-benzoylstaurosporine; PKC412

Application: PKC-412 is a broad spectrum tyrosine kinase inhibitor

CAS Number: 120685-11-2

Purity: ≥96%

Molecular Weight: 570.64

Molecular Formula: C₃₅H₃₀N₄O₄

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

* Refer to Certificate of Analysis for lot specific data (including water content).

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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.

References

1. Fabbro, D., et al. 2000. Anticancer Drug Des. 15: 17-28. PMID: 10888033
2. Weisberg, E., et al. 2002. Cancer Cell. 1: 433-443. PMID: 12124173
3. Stone, R.M., et al. 2005. Blood. 105: 54-60. PMID: 15345597
4. Li, H., et al. 2005. Nitric Oxide. 12: 231-236. PMID: 15890550
5. Chen, J., et al. 2005. Oncogene. 24: 8259-8267. PMID: 16091734

Physical State :

Solid

Solubility :

Soluble in DMSO (15 mg/ml), MDC (10 mg/ml), methanol (5 mg/ml), 100% ethanol (2.5 mg/ml), and DMF (20 mg/ml).

Storage :

Store at -20° C

Density :

1.48 g/cm³

Refractive Index :

n²⁰_D 1.77

IC50 :

MV4-11 (Myeloid leukemia cells): IC₅₀ = 12 nM (human); FLT3 ITD mutant autophosphorylation: IC₅₀ = 13 nM (human RS4-11 cells); Tyrosine-protein kinase receptor FLT3: IC₅₀ = 15 nM (human)

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

PubChem CID :

9829523

Merck Index :

14: 6185

MDL Number :

MFCD10687105

SMILES :

C[[email protected]@]12[[email protected]@H]([[email protected]@H](C[[email protected]@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)N(C)C(=O)C9=CC=CC=C9)OC

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Certificate of Analysis

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PKC-412 (CAS 120685-11-2) Product Citations

See how others have used PKC-412 (CAS 120685-11-2). Click on the entry to view the PubMed entry .

Citations 1 to 8 of 8 total

PMID: # 28403213 Hara, Y. et al. 2017. PLoS ONE. 12: e0175514.

PMID: # 28506695 Omori, I. et al. 2017. Exp. Hematol. 52: 56-64.e4.

PMID: # 28192400 Obata, Y. et al. 2017. Oncogene. 36: 3661-3672.

PMID: # 26771236 Fox, JM. et al. 2016. Oncotarget. 7: 7268-79.

PMID: # 27543462 Sulen, A. et al. 2016. Pharmacol. Res. 113: 216-227.

PMID: # 26104663 Peng, X. et al. 2015. Leukemia. 29: 2355-65.

PMID: # 24735609 Yoshida, A. et al. 2014. Biochem. Pharmacol. 90: 16-24.

PMID: # 25493654 Obata, Y. et al. 2014. Nat Commun. 5: 5715.

Citations 1 to 8 of 8 total

Rated 5 out of 5 by JT from Chen et al Chen et al. (PubMed ID 16091734) found that treatment of hematopoietic malignancies with the tyrosine kinase inhibitor, PKC-412, prevented the proliferation of hematopoietic Ba/F3 cells via FGFR3 regulation. -SCBT Publication Review

Date published: 2015-06-16

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