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Chemical Structure| 1800398-38-2 Chemical Structure| 1800398-38-2

Structure of LXH254
CAS No.: 1800398-38-2

Chemical Structure| 1800398-38-2

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LXH254 is an ATP-competitive inhibitor of Raf with anti-proliferative activity. Phase I.

Synonyms: Naporafenib

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Product Details of LXH254

CAS No. :1800398-38-2
Formula : C25H25F3N4O4
M.W : 502.49
SMILES Code : O=C(C1=CC(C(F)(F)F)=NC=C1)NC2=CC=C(C)C(C3=CC(OCCO)=NC(N4CCOCC4)=C3)=C2
Synonyms :
Naporafenib
MDL No. :MFCD31657408
InChI Key :UEPXBTCUIIGYCY-UHFFFAOYSA-N
Pubchem ID :90456533

Safety of LXH254

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of LXH254

MAPK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
BRAFV600E 1 nM 30 min Evaluate the inhibitory effect of Tovorafenib on BRAFV600E PMC10149214
BRAFWT 1 nM 30 min Evaluate the inhibitory effect of Tovorafenib on BRAFWT PMC10149214
ARAFSSDD 10 nM 30 min Evaluate the inhibitory effect of Tovorafenib on ARAFSSDD PMC10149214
CRAFWT 4 nM 30 min Evaluate the inhibitory effect of Tovorafenib on CRAFWT PMC10149214
MCF10AecoR cells 1 µM 4 hours To study the effect of mTOR inhibitors on BRAF T401 phosphorylation, results showed rapamycin partially suppressed pT401 levels. PMC11370054
HEK293T cells 1 µM 4 hours To evaluate the effect of ACBI1 on SMARCA4 protein levels in HEK293T cells, results showed that ACBI1 treatment led to a reduction in SMARCA4 protein levels. PMC11370054
WM3928 cells 1 µM 6 hours To study the effect of mTOR inhibitors on BRAF T401 phosphorylation, results showed dactolisib significantly suppressed pT401 levels. PMC11370054
CRAFSSDD 1 nM 30 min Evaluate the inhibitory effect of Tovorafenib on CRAFSSDD PMC10149214

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03333343 EGFR-mutant Non-small Cell Lun... More >>g Cancer Less << Phase 1 Recruiting May 21, 2021 Canada, Ontario ... More >> Novartis Investigative Site Recruiting Toronto, Ontario, Canada, M5G 2M9 Germany Novartis Investigative Site Recruiting Koeln, Germany, 50937 Italy Novartis Investigative Site Recruiting Ancona, AN, Italy, 60126 Novartis Investigative Site Recruiting Milano, MI, Italy, 20162 Singapore Novartis Investigative Site Recruiting Singapore, Singapore, 169610 Taiwan Novartis Investigative Site Recruiting Tainan, Taiwan, 70421 Novartis Investigative Site Recruiting Taipei, Taiwan, 10002 Less <<
NCT02974725 Non-Small Cell Lung Cancer ... More >> Melanoma Less << Phase 1 Recruiting June 29, 2020 United States, Massachusetts ... More >> Novartis Investigative Site Recruiting Boston, Massachusetts, United States, 02114 Contact: Bakhan Barzangy    617-726-1849    bbarzangy@mgh.harvard.edu    Principal Investigator: Rebecca Heist          Australia, Victoria Novartis Investigative Site Recruiting Melbourne, Victoria, Australia, 3000 Belgium Novartis Investigative Site Recruiting Leuven, Belgium, 3000 France Novartis Investigative Site Recruiting Villejuif Cedex, France, 94805 Germany Novartis Investigative Site Recruiting Frankfurt, Germany, 60590 Novartis Investigative Site Recruiting Koeln, Germany, 50937 Italy Novartis Investigative Site Recruiting Rozzano, MI, Italy, 20089 Spain Novartis Investigative Site Recruiting Barcelona, Catalunya, Spain, 08036 Less <<
NCT02607813 NSCLC Ovarian... More >> Cancer Melanoma Other Solid Tumors Less << Phase 1 Recruiting December 16, 2019 United States, Massachusetts ... More >> Novartis Investigative Site Recruiting Boston, Massachusetts, United States, 02114 United States, New York Novartis Investigative Site Recruiting New York, New York, United States, 10021 Contact: Alida Beck       becka@mskcc.org    Principal Investigator: Gopakumar Iyer          United States, Texas UT M.D Anderson Cancer Center SC - LXH254X2101 Recruiting Houston, Texas, United States, 77030 Contact: Zehra Maloo    713-563-4426    zmaloo@mdanderson.org    Principal Investigator: Filip Janku          Canada, Ontario Novartis Investigative Site Recruiting Toronto, Ontario, Canada, M6G 1Z5 France Novartis Investigative Site Recruiting Paris, France, 75010 Novartis Investigative Site Recruiting Toulouse Cedex 9, France, 31059 Germany Novartis Investigative Site Recruiting Essen, Germany, 45147 Novartis Investigative Site Recruiting Heidelberg, Germany, 69120 Japan Novartis Investigative Site Recruiting Chuo-ku, Tokyo, Japan, 104-0045 Korea, Republic of Novartis Investigative Site Recruiting Seoul, Korea, Korea, Republic of, 03080 Netherlands Novartis Investigative Site Recruiting Groningen, Netherlands, 9713 GZ Contact: Department of Pulmonary Diseases University Medical Center Groningen    +31 503611546    h.j.m.groen@umcg.nl    Principal Investigator: H.J.M. Groen, M.D.          Medical Oncology, Erasmus MC Recruiting Rotterdam, Netherlands, 3075 CE Contact       m.dejonge@erasmusmc.nl    Principal Investigator: M. de Jonge, M.D.          Spain Novartis Investigative Site Recruiting Barcelona, Catalunya, Spain, 08035 Novartis Investigative Site Recruiting Madrid, Spain, 28007 Switzerland Novartis Investigative Site Recruiting Zuerich, Switzerland, 8091 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.95mL

1.99mL

1.00mL

19.90mL

3.98mL

1.99mL

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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