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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
M233 500 nM 24 h inhibition of pRSK, rebound in pERK1/2, increase in pMEK Mol Cancer. 2014 Aug 20;13:194.
M238 500 nM 24 h inhibition of pRSK and pERK1/2, reduction in pAKT levels, slight induction of pMEK Mol Cancer. 2014 Aug 20;13:194.
M262 500 nM 24 h inhibition of pRSK and pERK1/2, reduction in pAKT levels Mol Cancer. 2014 Aug 20;13:194.
M381 500 nM 24 h induction of pMEK and pERK1/2, no change in pRSK Mol Cancer. 2014 Aug 20;13:194.
M409 500 nM 24 h inhibition of pRSK, reduction in pERK1/2, increase in pMEK Mol Cancer. 2014 Aug 20;13:194.
Hep3B cells 10 μM 24 h SCH772984 suppressed the LAGE3 upregulation-induced proliferation, migration, and invasion of Hep3B cells. Cell Mol Biol Lett. 2021 Nov 27;26(1):49.

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. J Exp Clin Cancer Res. 2022 Oct 13;41(1):301

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

References

 

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