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Chemical Structure| 1454682-72-4 Chemical Structure| 1454682-72-4

Structure of LY3009120
CAS No.: 1454682-72-4

Chemical Structure| 1454682-72-4

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LY3009120 (DP-4978) is a pan RAF inhibitor that inhibits BRAFV600E, BRAFWT, and CRAFWT with IC50 values of 5.8 nM, 9.1 nM, and 15 nM, respectively.

Synonyms: DP-4978

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Product Details of LY3009120

CAS No. :1454682-72-4
Formula : C23H29FN6O
M.W : 424.51
SMILES Code : O=C(NC1=CC(C2=CC3=CN=C(NC)N=C3N=C2C)=C(C)C=C1F)NCCC(C)(C)C
Synonyms :
DP-4978
MDL No. :MFCD28411374
InChI Key :HHCBMISMPSAZBF-UHFFFAOYSA-N
Pubchem ID :71721540

Safety of LY3009120

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

Related Pathways of LY3009120

MAPK

Isoform Comparison

Biological Activity

Target
  • B-Raf

    BRAF(V600E), IC50:5.8 nM

    BRAF WT, IC50:15 nM

  • C-Raf/Raf-1

    C-Raf, IC50:4.3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
WM1366 1μM 48 hours The combination of LY3009120 with sorafenib and aspirin blocked hyperactivation of ERK signaling without inhibiting AMPK pathway activity. PMC5844814
A549 1μM 48 hours The combination of LY3009120 with sorafenib and aspirin blocked hyperactivation of ERK signaling without inhibiting AMPK pathway activity. PMC5844814
K1 cells 5 μM and 10 μM 48 hours LY3009120 successfully overcame Vemurafenib resistance and suppressed the growth of DTC cells in vitro and in vivo. PMC5381260
BCPAP cells 5 μM and 10 μM 48 hours LY3009120 successfully overcame Vemurafenib resistance and suppressed the growth of DTC cells in vitro and in vivo. PMC5381260
KTC-1 cells 5 μM and 10 μM 48 hours LY3009120 successfully overcame Vemurafenib resistance and suppressed the growth of DTC cells in vitro and in vivo. PMC5381260
H/N/KRAS-less MEFs 0, 0.003, 0.03, 0.3, 3.0 μM 24 hours LY3009120 induced increased ERK phosphorylation and Cyclin D1 expression in H/N/KRAS-less MEFs. PMC8812530
SKMEL239 15 nM 1 hour Inhibition of ERK1/2 phosphorylation PMC11825127
SKMEL239-C4 27 nM 1 hour Inhibition of ERK1/2 phosphorylation PMC11825127

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
nude mice K1 cell xenograft model subcutaneous injection 100 mg/kg or 200 mg/kg Once daily for three weeks followed by one week off LY3009120 monotherapy or combination therapy with Obatoclax significantly suppressed tumor growth in the thyroid cancer xenograft model. PMC5381260

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.78mL

2.36mL

1.18mL

23.56mL

4.71mL

2.36mL

References

 

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