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Substance Name: Amuvatinib [USAN:INN]
RN: 850879-09-3
UNII: SO9S6QZB4R
InChIKey: FOFDIMHVKGYHRU-UHFFFAOYSA-N

Note

  • c-Kit/AXL tyrosine kinase inhibitor that synergizes with docetaxel (taxotere) and is cytotoxic to gastrointestinal stromal tumor cells.

    NCI: An orally bioavailable synthetic carbothioamide with potential antineoplastic activity. Amuvatinib binds to mutant forms of the stem cell factor receptor (c-Kit; SCFR), inhibiting clinically relevant mutants of this receptor tyrosine kinase that may be associated with resistance to therapy. In addition, amuvatinib inhibits activities of other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3 and PDGFR alpha, which are frequently dysregulated in variety of tumors. This agent also suppresses the induction of DNA repair protein Rad51, thereby potentiating the activities of DNA damage-inducing agents. Mutant forms of c-Kit are often associated with tumor chemoresistance. (NCI Thesaurus)

Molecular Formula

  • C23-H21-N5-O3-S

Molecular Weight

  • 447.5169
 

Classification Code

  • Treatment of Cancer
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Names and Synonyms

Name of Substance

  • Amuvatinib [USAN:INN]

Synonyms

  • Amuvatinib
  • HPK56
  • MP-470
  • MP470
  • N-(1,3-Benzodioxol-5-ylmethyl)-4-(benzofuro(3,2-d)pyrimidin-4-yl)piperazine-1- carbothioamide
  • UNII-SO9S6QZB4R

Systematic Name

  • 1-Piperazinecarbothioamide, N-(1,3-benzodioxol-5-ylmethyl)-4-benzofuro(3,2-d)pyrimidin-4-yl-

Registry Numbers

CAS Registry Number

  • 850879-09-3

FDA UNII

  • SO9S6QZB4R

System Generated Number

  • 0850879093

Structure Descriptors

InChI

1S/C23H21N5O3S/c32-23(24-12-15-5-6-18-19(11-15)30-14-29-18)28-9-7-27(8-10-28)22-21-20(25-13-26-22)16-3-1-2-4-17(16)31-21/h1-6,11,13H,7-10,12,14H2,(H,24,32)

InChIKey

FOFDIMHVKGYHRU-UHFFFAOYSA-N

Smiles

S=C(NCc1ccc2OCOc2c1)N3CCN(CC3)c4ncnc5c4oc6ccccc56