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Chemical Structure| 942183-80-4 Chemical Structure| 942183-80-4

Structure of SCH772984
CAS No.: 942183-80-4

Chemical Structure| 942183-80-4

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SCH772984 is a highly selective and ATP-competitive ERK inhibitor with IC50 values of 4 nM and 1 nM for ERK1 and ERK2, respectively. It has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.

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Product Details of SCH772984

CAS No. :942183-80-4
Formula : C33H33N9O2
M.W : 587.67
SMILES Code : O=C([C@H]1CN(CC(N2CCN(C3=CC=C(C4=NC=CC=N4)C=C3)CC2)=O)CC1)NC5=CC6=C(NN=C6C7=CC=NC=C7)C=C5
MDL No. :MFCD28144700
InChI Key :HDAJDNHIBCDLQF-RUZDIDTESA-N
Pubchem ID :24866313

Safety of SCH772984

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of SCH772984

MAPK

Isoform Comparison

Biological Activity

Target
  • ERK2

    ERK2, IC50:1 nM

  • ERK1

    ERK1, IC50:4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
M262 500 nM 24 h Inhibition of pRSK and pERK1/2, reduction in pAKT levels PMC4155088
M233 500 nM 24 h Inhibition of pRSK, rebound in pERK1/2, increase in pMEK PMC4155088
M238 500 nM 24 h Inhibition of pRSK and pERK1/2, reduction in pAKT levels, slight induction of pMEK PMC4155088
M381 500 nM 24 h Induction of pMEK and pERK1/2, no change in pRSK PMC4155088
M409 500 nM 24 h Inhibition of pRSK, reduction in pERK1/2, increase in pMEK PMC4155088
Hep3B cells 10 μM 24 h SCH772984 suppressed the LAGE3 upregulation-induced proliferation, migration, and invasion of Hep3B cells. PMC8903694

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Breast cancer xenograft model Intraperitoneal injection 25 mg/kg Twice daily for 2 weeks To evaluate the inhibitory effect of ERK1/2 inhibitor SCH772984 on breast cancer metastasis and CTC formation. The results showed that SCH772984 significantly reduced CTC numbers and lung metastasis. PMC9558416

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.51mL

1.70mL

0.85mL

17.02mL

3.40mL

1.70mL

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