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Regorafenib (BAY 73-4506)

Catalog No.S1178
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Regorafenib (BAY 73-4506) Chemical Structure

  • Linifanib (ABT-869)

    Linifanib (ABT869) is a structurally novel, potent RTK and VEGF and PDGF receptor families inhibitor for, PDGFR-β, KDR, and CSF-1R, with IC50 of 0.2 nM, 2 nM, 4 nM, and 7 nM, respectively.

  • Axitinib

    Axitinib (AG-013736) is a multiple receptor kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β and c-KIT with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.

  • BIBF1120 (Vargatef)

    BIBF1120 (Vargatef) is a potent VEGF receptor (VEGFR), PDGFR and FGFR kinase inhibitor for VEGFR1, VEGFR2, VEGFR3 with IC50 of 34 nM, 5 nM and 5 nM, respectively.

  • Cediranib (AZD2171)

    Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor for VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 nM and 0.5 nM, respectively.

  • Dovitinib (TKI-258)

    Dovitinib(TKI-258) is a highly potent, novel multitargeted growth factor receptor kinase inhibitor with IC50 of 1, 2, 5, 10, 8, 27, 36 nM for FLT3, c-KIT, FGFR, VEGFR1/2/3, PDGFRß and CSF-1R, respectively.

  • Dasatinib (BMS-354825)

    Dasatinib also known as BMS-354825, Sprycel, BMS354825 is ATP-competitive, dual SRC/ABL inhibitor. BMS-354825 inhibits all members of the Src family, including c-Src, Lck, Fyn, and Yes (IC50 < 1.1nmol/L).

  • Imatinib Mesylate

    Imatinib Mesylate is a multitargeted c-kit, PDGF-R and c-ABL inhibitor with IC50 of 3.9 and 2.9 μM for the inhibition of T-cell proliferation stimulated by DCs and PHA, respectively.

  • Motesanib Diphosphate (AMG-706)

    Motesanib (AMG-706) is a multiple inhibitor of VEGFR1/2/3(IC50: 2 ηM /3 ηM /6 ηM),PDGFR (84ηM), kit (8ηM), and Ret (59ηM)receptors

  • Pazopanib HCl

    Pazopanib HCl is a VEGFR inhibitor, IC50 of 10, 30 and 47 nM for VEGFR-1, -2, and -3.

  • Sorafenib (Nexavar)

    Sorafenib (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.

Biological Activity

Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature. Regorafenib (BAY 73-4506) binds to and inhibits VEGFR-2 and -3, and tumor cell signaling kinases (RET, KIT, PDGFR, and Raf), which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. Regorafenib (BAY 73-4506) shows potent, oral activity in a wide variety of preclinical xenograft models. [1]

References on Regorafenib (BAY 73-4506)
  • [1] International Journal of Cancer 2011;129:245-255
Molecular Weight (WM): 482.82
Formula:

C21H15ClF4N4O3

CAS No.: 755037-03-7
Synonyms:
N/A
Dissolve in (25°C): DMSO ≥97mg/mL 
Water <1mg/mL 
Ethanol ≥8mg/mL 
Storage: 2 years-20°CPowder
1 week-4°Cin DMSO
1 month-80°in DMSO

Quality Control & MSDS

View current batch:
COA H-NMR HPLC COA H-NMR HPLC
Notes:

Related Inhibitors

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