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HomeProduct name listSCH772984

SCH772984

  • CAS NO.:942183-80-4
  • Empirical Formula: C33H33N9O2
  • Molecular Weight: 587.67
  • MDL number: MFCD11878503
  • EINECS: 1592732-453-0
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-11-19 20:33:22
SCH772984 Structural

What is SCH772984?

Description

The extracellular regulated kinases 1 and 2 (ERK1/2) are functionally redundant kinases activated by a variety of growth factors and mitogens. SCH 772984 is a potent inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively). It is highly selective, with only seven kinases of 300 tested showing more than 50% inhibition at a concentration of 1 μM. SCH 772984 has nanomolar cytotoxicity in tumor cells with mutations in BRAF, NRAS, or KRAS. It is effective in vivo, inducing regression of xenograft tumors in mice. SCH 772984 displays slow binding kinetics, binding to a novel binding pocket in inactive ERK isoforms.

The Uses of SCH772984

SCH772984 is a novel and selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors and has nanomolar cellular potency in tumor cells with mutations in BRAF, NRA5, or KRAS and induces tumor regressions in xenograft models.

Definition

ChEBI: SCH772984 is a member of the class of indazoles that is 1H-indazole substituted by pyridin-4-yl and {[(3R)-1-(2-oxo-2-{4-[4-(pyrimidin-2-yl)phenyl]piperazin-1-yl}ethyl)pyrrolidin-3-yl]carbonyl}amino groups at positions 3 and 5, respectively. It is a potent inhibitor of mitogen-activated protein kinases ERK1 and ERK2 (IC50 = 4 and 1 nM, respectively) that exhibits anti-cancer properties. It has a role as an antineoplastic agent, an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, an apoptosis inducer and an analgesic. It is a member of pyridines, a biaryl, a secondary carboxamide, a pyrrolidinecarboxamide, a member of indazoles, a tertiary amino compound, a N-acylpiperazine, a N-arylpiperazine, a member of pyrimidines, a N-alkylpyrrolidine and a tertiary carboxamide.

What are the applications of Application

SCH772984 is a novel and selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors and has nanomolar cellular potency in tumor cells

Properties of SCH772984

Melting point: >214°C (dec.)
Boiling point: 857.3±65.0 °C(Predicted)
Density  1.353±0.06(20.0000℃)
storage temp.  Refrigerator
solubility  DMSO (Slightly)
pka 12.05±0.40(Predicted)
form  Solid
color  Pale Yellow
CAS DataBase Reference 942183-80-4

Safety information for SCH772984

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for SCH772984

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