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Chemical Structure| 1453848-26-4 Chemical Structure| 1453848-26-4

Structure of Ravoxertinib
CAS No.: 1453848-26-4

Chemical Structure| 1453848-26-4

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Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor, with IC50 values of 6.1 nM for ERK1 and 3.1 nM for ERK2.

Synonyms: GDC-0994; RG-7842

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Product Details of Ravoxertinib

CAS No. :1453848-26-4
Formula : C21H18ClFN6O2
M.W : 440.86
SMILES Code : O=C1C=C(C2=NC(NC3=CC=NN3C)=NC=C2)C=CN1[C@@H](C4=CC=C(Cl)C(F)=C4)CO
Synonyms :
GDC-0994; RG-7842
MDL No. :MFCD28143918
InChI Key :RZUOCXOYPYGSKL-GOSISDBHSA-N
Pubchem ID :71727581

Safety of Ravoxertinib

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

Related Pathways of Ravoxertinib

MAPK

Isoform Comparison

Biological Activity

Target
  • ERK2

    ERK2, IC50:0.3 nM

  • ERK1

    ERK1, IC50:1.1 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
early osteoclast precursors (OCPs) 110 nM 8 hours Inhibited ERK pathway, reduced IL-4-induced proliferation of early osteoclast precursors PMC8642926
FaDu cells 100 nM 24, 48, 72 hours To evaluate the inhibitory effect of Ravoxertinib on Erk1/2 phosphorylation, results showed that Ravoxertinib significantly inhibited Erk1/2 phosphorylation and reduced erastin-induced lipid peroxidation and ROS production. PMC9856753
SCC25 cells 100 nM 24, 48, 72 hours To evaluate the inhibitory effect of Ravoxertinib on Erk1/2 phosphorylation, results showed that Ravoxertinib significantly inhibited Erk1/2 phosphorylation and reduced erastin-induced lipid peroxidation and ROS production. PMC9856753
KHM-5M 0.03 μM, 0.1 μM, 1 μM 0.5 hours, 24 hours GDC-0994 inhibited RSK phosphorylation, and this inhibition was more significant in BRAF mutant cells PMC11107342
SH-SY5Y cells 100 nM 96 hours ravoxertinib at 100 nM was less toxic than PD0325901 at 5 nM concentration, while ravoxertinib induced much stronger ERK inhibition PMC9358475
LNCaP cells 7.5 μM 48 hours To evaluate the effect of AS602801 combined with Enzalutamide on the viability of LNCaP cells, the results showed that the combination significantly reduced cell viability. PMC7082632
C4-2 cells 7.5 μM 48 hours To evaluate the effect of AS602801 combined with Enzalutamide on the viability of C4-2 cells, the results showed that the combination significantly reduced cell viability. PMC7082632
22Rv1 cells 7.5 μM 48 hours To evaluate the effect of AS602801 combined with Enzalutamide on the viability of 22Rv1 cells, the results showed that the combination significantly reduced cell viability. PMC7082632

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice KRASG12D mutant mouse model Oral Once daily for 4 weeks Reversed lymphangiectasia and improved survival PMC9536262
mice CRC bone metastasis model intratibial injection 2 mg/kg Once daily for 7 days Inhibited ERK pathway, significantly restored bone volume and prevented osteoclast activation PMC8642926
BALB/c nude mice BRAF mutant xenograft model oral gavage 40 μg Twice daily for 5 days GDC-0994 nearly completely abolished the growth of BRAF mutant xenografts, but had no significant effect on wild-type tumors PMC11107342
BALB/c nude mice Subcutaneous tumor model Injection 10 mg/kg once a week, for three weeks To investigate the function of circRNA-0044301 in vivo, it was found that interference with circRNA-0044301 significantly reduced tumor volume. PMC9454757
nude mice LNCaP xenograft model intraperitoneal injection 25 mg/kg once daily for 2 weeks To evaluate the effect of AS602801 combined with Enzalutamide on tumor growth in the LNCaP xenograft model, the results showed that the combination significantly suppressed tumor growth. PMC7082632

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.34mL

2.27mL

1.13mL

22.68mL

4.54mL

2.27mL

References

 

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