Molecular structure of Tozasertib, CAS Number: 639089-54-6
Tozasertib (CAS 639089-54-6)
See product citations (4)
Alternate Names:
MK0457; VX 680; MK 0457
Application:
Tozasertib is a potent and selective pan-ARK inhibitor
CAS Number:
639089-54-6
Purity:
≥98%
Molecular Weight:
464.59
Molecular Formula:
C23H28N8OS
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Product Citations
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
Tozasertib is a potent pan-ARK inhibitor but favors ARK-1 (Ki = 0.6 nM) over ARK-2 (Ki = 18 nM) or ARK-3 (Ki = 4.6 nM). It shows selectivity against a panel of more than 190 different protein kinases. Tozasertib effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50 < 10muM), inhibiting H3 histone phosphorylation and increasing apoptosis. By depleting ARK activity, tozasertib disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase.
Tozasertib (CAS 639089-54-6) References
- Discovery and development of aurora kinase inhibitors as anticancer agents. | Pollard, JR. and Mortimore, M. 2009. J Med Chem. 52: 2629-51. PMID: 19320489
- VX680/MK-0457, a potent and selective Aurora kinase inhibitor, targets both tumor and endothelial cells in clear cell renal cell carcinoma. | Li, Y., et al. 2010. Am J Transl Res. 2: 296-308. PMID: 20589168
- Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class. | Salah, E., et al. 2011. J Med Chem. 54: 2359-67. PMID: 21417343
- ABCG2 impairs the activity of the aurora kinase inhibitor tozasertib but not of alisertib. | Michaelis, M., et al. 2015. BMC Res Notes. 8: 484. PMID: 26415506
- Tozasertib attenuates neuronal apoptosis via DLK/JIP3/MA2K7/JNK pathway in early brain injury after SAH in rats. | Yin, C., et al. 2016. Neuropharmacology. 108: 316-23. PMID: 27084696
- RIPK1-dependent cell death: a novel target of the Aurora kinase inhibitor Tozasertib (VX-680). | Martens, S., et al. 2018. Cell Death Dis. 9: 211. PMID: 29434255
- Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy. | Rossari, F., et al. 2018. J Hematol Oncol. 11: 84. PMID: 29925402
- Aurora kinase inhibitor tozasertib suppresses mast cell activation in vitro and in vivo. | Zhang, LN., et al. 2020. Br J Pharmacol. 177: 2848-2859. PMID: 32017040
- Tozasertib Attenuates Neuropathic Pain by Interfering with Aurora Kinase and KIF11 Mediated Nociception. | Uniyal, A., et al. 2021. ACS Chem Neurosci. 12: 1948-1960. PMID: 34027667
- Reversing tozasertib resistance in glioma through inhibition of pyruvate dehydrogenase kinases. | Jane, EP., et al. 2022. Mol Oncol. 16: 219-249. PMID: 34058053
- Inhibition of pan-Aurora kinase attenuates evoked and ongoing pain in nerve injured rats via regulating KIF17-NR2B mediated signaling. | Uniyal, A., et al. 2022. Int Immunopharmacol. 106: 108622. PMID: 35183034
- Modulation of KIF17/NR2B crosstalk by tozasertib attenuates inflammatory pain in rats. | Uniyal, A., et al. 2022. Inflammopharmacology. 30: 549-563. PMID: 35243557
- Single-cell profiling reveals molecular basis of malignant phenotypes and tumor microenvironments in small bowel adenocarcinomas. | Yang, J., et al. 2022. Cell Discov. 8: 92. PMID: 36104333
Inhibitor of:
4930404A10Rik, ACCα, APC15, APC4, APC5, APC8, ARHGAP36, ARHGAP40, ARHGEF15, ARHGEF5_Arhgef5, ARK, ARK-1, ARK-2, ARK-3, AURA1, Aurora, BC024659, BC057079, Bora, Bub2, C12orf28, C18orf15, C20orf26, C230052I12Rik, C230055K05Rik, C5orf55, CASC5, CENP-R, CENP-T, CENPBD1, Centaurin γ3, centlein, Centrin, Centriolin, CEP152, CLASP (Cytoplasmic Linker Associated Protein), CPSF4L, CSN3, CXXC5, DDX21, DOCK 7, DPRP, Dtl, EG244495, EG620736, FEM-3, FLJ44815, FMIP, Frabin, fzr, Gpa2, GPB5, hCAP-H, IL-1F7, Ini1, INSC, IRF-2BP1, KIF (Kinesin family), KLHDC9, KNL2, LARG, LOC100041206, LOC100041228, LOC100041378, LOC342918, MAD2_Mad2, MARCO, MIC1, MIS12, MKLP-1, Mog1p, MPHOSPH8, MYEOV2, NLR family CARD domain-containing (NLRC), p73β, PARD3A, PCBP4, PICH_Ercc6l, Rab 27b, Rad59, Ral GPS1, RbAp48, Rbx1, Rho 8, Rho F, RIOK1, RIP/Rab, RMP, SCAI, Sgo1, Six6os1, Speedy E5, Srb7, STH1, STK31, String, TAF II p170, Taspase 1, TBC1D10B, THA1, Tiam2, TopBP1, TPX2, TRB-1, TRIP13, WDR24, WDR26, ZNF490, ZNF491, ZNF493, ZNF526, ZNF529, ZNF534, and ZNF543.Activator of:
ARHGAP39, ARHGEF38, BUB1, BUB3, BUBR1, C10orf104, C14orf106, Cdc5, CENP-I, CENP-T, CEP72, DEK, Hec1, Histone cluster 1 H1T, MASTL, Mps1, Nek7, NSL1, RCC2, Rho GAP p190-B, RICH2, RNA pol α, Sororin, and Spc25.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Tozasertib, 25 mg | sc-358750 | 25 mg | $61.00 | |||
Tozasertib, 50 mg | sc-358750A | 50 mg | $85.00 |