product name XMD8-92
Description: XMD8-92 is a novel, potent and selective BMK1/ERK5 inhibitor with Kd of 80 nM, it less potently inhibits DCAMKL2, TNK1, and Plk4 (Kds of 190, 890, and 600 nM, respectively). XMD8-92 inhibits pancreatic tumor xenograft growth via a DCLK1-dependent mechanism. ERK5 pathway regulates transcription factors important for monocytic differentiation of human myeloid leukemia cells.
References: Cancer Cell. 2010 Sep 14;18(3):258-67; Cancer Lett. 2014 Aug 28;351(1):151-61.
474.55
Formula
C26H30N6O3
CAS No.
1234480-50-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 73 mg/mL (153.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19415354
| In Vitro |
In vitro activity: XMD8-92, via inhibition of BMK1 activation, significantly induces p21 expression in cells, and mediates suppression of cancer cell proliferation. XMD8-92 markedly abrogates the inhibitive effects of hydroxysafflor yellow A (HSYA) on hepatic stellate cell (HSC) activation, and blockes the HSYA-mediated MEF2C down-regulation. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | XMD8-92 (50 mg/kg i.p.) significantly inhibit the growth of the xenografted human or syngeneic mouse tumors by blocking tumor cell proliferation and tumor-associated angiogenesis. XMD8-92 inhibits pancreatic tumor xenograft growth by significant downregulation of DCLK1 and several of its downstream targets |
| Animal model | mouse |
| Formulation & Dosage | 50 mg/kg; i.p. |
| References | Cancer Cell. 2010 Sep 14;18(3):258-67; Cancer Lett. 2014 Aug 28;351(1):151-61. |
