About: BMS-354825   Sponge Permalink

An Entity of Type : dbkwik:resource/rq8Z6H1D5ZQ6xf9ogWx0pw==, within Data Space : 134.155.108.49:8890 associated with source dataset(s)

It is a highly potent of both BCR-ABL and Src kinases in sub-nanomolar concentrations, and serves as a polypharmacological dual inhibitor, thus relaxing its structural binding specificity to ABL and increasing tolerance to point amino acid mutations that would otherwise confer resistance to other kinase inhibitors; BMS-354825's characteristics allow it to override the M244V, G250E, Q252H, Q252R, Y253F, Y253H, E255K, E255V, F317L, M351T, E355G, F359V, H396R, and F486S mutations in ABL that otherwise confer resistance to imantinib, thus demonstrating its clinical relevance.

AttributesValues
rdf:type
rdfs:label
  • BMS-354825
rdfs:comment
  • It is a highly potent of both BCR-ABL and Src kinases in sub-nanomolar concentrations, and serves as a polypharmacological dual inhibitor, thus relaxing its structural binding specificity to ABL and increasing tolerance to point amino acid mutations that would otherwise confer resistance to other kinase inhibitors; BMS-354825's characteristics allow it to override the M244V, G250E, Q252H, Q252R, Y253F, Y253H, E255K, E255V, F317L, M351T, E355G, F359V, H396R, and F486S mutations in ABL that otherwise confer resistance to imantinib, thus demonstrating its clinical relevance.
side
  • Minimal side-effects
dbkwik:halo-fanon/...iPageUsesTemplate
dbkwik:halofanon/p...iPageUsesTemplate
Molweight
  • 488(xsd:double)
Solubility
  • DMSO
Name
  • BMS-354825
Chemformula
  • C22H26ClN7O2S
Mechanism
  • *BCR-ABL inhibitor, IC50 < 1.0 nM *Src inhibitor, IC50 = 0.50 nM *Lck inhibitor, IC50 = 0.40 nM *Yes inhibitor, IC50 = 0.50 nM
Clinuse
  • Chronic myelogenous leukemia anticancer drug
Bioavail
  • High
Marketed
IUPAC name
  • N--2-thiazole-5-carboxamide
Halflife
  • High
Legal
  • Approved for clinical usage by the UNSC Medical Corps
Route
  • *Oral *Intravenous
abstract
  • It is a highly potent of both BCR-ABL and Src kinases in sub-nanomolar concentrations, and serves as a polypharmacological dual inhibitor, thus relaxing its structural binding specificity to ABL and increasing tolerance to point amino acid mutations that would otherwise confer resistance to other kinase inhibitors; BMS-354825's characteristics allow it to override the M244V, G250E, Q252H, Q252R, Y253F, Y253H, E255K, E255V, F317L, M351T, E355G, F359V, H396R, and F486S mutations in ABL that otherwise confer resistance to imantinib, thus demonstrating its clinical relevance.
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