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Chemical Structure| 1446090-79-4 Chemical Structure| 1446090-79-4

Structure of Lifirafenib
CAS No.: 1446090-79-4

Chemical Structure| 1446090-79-4

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In vitro, BGB-283 potently inhibits BRAFV600E-activated ERK phosphorylation and cell proliferation.

Synonyms: BGB-283; Beigene-283

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Product Details of Lifirafenib

CAS No. :1446090-79-4
Formula : C25H17F3N4O3
M.W : 478.42
SMILES Code : O=C1NC2=C(C(OC3=CC=C(O[C@@]4([H])[C@]5([H])[C@@H]4C6=NC7=CC=C(C(F)(F)F)C=C7N6)C5=C3)=CC=N2)CC1
Synonyms :
BGB-283; Beigene-283
MDL No. :MFCD30489379

Safety of Lifirafenib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Lifirafenib

MAPK

Isoform Comparison

Biological Activity

Target
  • EGFR/ErbB1

    EGFR, IC50:29 nM

  • mutant EGFR

    EGFR(T790M/L858R), IC50:495 nM

  • B-Raf

    BRAF WT, IC50:32 nM

    BRAF(V600E), IC50:23 nM

  • C-Raf/Raf-1

    C-RAF (Y340/341D), IC50:7 nM

  • A-raf

    WT A-RAF, IC50:1 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HCC364 (BRAF V600E mutation) 0.64 nM to 10 μM 72 hours Evaluate the inhibitory effect of Lifirafenib on BRAF V600E mutant cells, IC50: <1.0-27.0nM PMC7529990
H1755 (BRAF G469A mutation) 0.64 nM to 10 μM 72 hours Evaluate the inhibitory effect of Lifirafenib on BRAF G469A mutant cells, IC50: 3.5-25.7nM PMC7529990
H2087 (BRAF L597V mutation) 0.64 nM to 10 μM 72 hours Evaluate the inhibitory effect of Lifirafenib on BRAF L597V mutant cells, IC50: 3.5-25.7nM PMC7529990
SK-MEL-239 cells 1 µM 1 h Evaluate the inhibitory effect of BGB-283 on ERK phosphorylation in SK-MEL-239 cells, showing BGB-283 effectively inhibits ERK phosphorylation PMC7400788
Calu-6 cells 1 µM 1 h Evaluate the inhibitory effect of BGB-283 and selumetinib combination on Calu-6 cell proliferation, showing BGB-283 significantly enhances the antiproliferative activity of selumetinib PMC7400788

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Calu-6 NSCLC xenograft model Oral gavage 5-15 mg/kg Twice daily for 28 days Evaluate the antitumor effect of BGB-283 and selumetinib combination in Calu-6 xenograft model, showing combination therapy significantly enhances antitumor activity PMC7400788

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03641586 Solid Tumors PHASE1 COMPLETED 2019-03-07 Beijing Cancer Hospital, Beiji... More >>ng, Beijing, 100142, China Less <<
NCT02610361 Solid Tumors PHASE1 COMPLETED 2025-10-17 Chris Obrien Lifehouse, Camper... More >>down, New South Wales, 2050, Australia|North Coast Cancer Institute, Macquarie, New South Wales, 2444, Australia|Prince of Wales Hospital, Randwick, New South Wales, 2031, Australia|Westmead Hospital, Westmead, New South Wales, 2145, Australia|Princess Alexandra Hospital, Brisbane, Queensland, 4102, Australia|Tasman Oncology Research Ltd, Southport Gold Coast, Queensland, 4216, Australia|Royal Adelaide Hospital, Adelaide, South Australia, 5000, Australia|Box Hill Hospital, Box Hill, Victoria, 3128, Australia|Monash Health, Clayton, Victoria, 3168, Australia|Austin Health, Heidelberg, Victoria, 3084, Australia|Cabrini Hospital Malvern, Malvern, Victoria, 3144, Australia|Peter Maccallum Cancer Centre, Melbourne, Victoria, 3000, Australia|Alfred Cancer Trials, Melbourne, Victoria, 3004, Australia|Royal Melbourne Hospital, Parkville, Victoria, 3052, Australia|Linear Clinical Research, Nedlands, Western Australia, 6009, Australia|Christchurch Hospital, Christchurch, 8011, New Zealand|Dunedin Hospital, Dunedin, 9016, New Zealand|Waikato Hospital, Hamilton Waikato, 3204, New Zealand|Wellington Regional Hospital (Ccdhb), Wellington, 6021, New Zealand Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.45mL

2.09mL

1.05mL

20.90mL

4.18mL

2.09mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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