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Chemical Structure| 1096708-71-2 Chemical Structure| 1096708-71-2

Structure of Tovorafenib
CAS No.: 1096708-71-2

Chemical Structure| 1096708-71-2

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Tovorafenib (TAK-580, MLN 2480) is an oral, selective, broad-spectrum inhibitor of Raf. Tovorafenib (TAK-580, MLN 2480) acts by counteracting the feedback activation of MEK triggered by TAK-733, resulting in more coordinated inhibition of the MAPK pathway.

Synonyms: TAK-580; MLN2480; BUB 024

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Product Details of Tovorafenib

CAS No. :1096708-71-2
Formula : C17H12Cl2F3N7O2S
M.W : 506.29
SMILES Code : O=C(C1=CN=C([C@H](NC(C2=NC=NC(N)=C2Cl)=O)C)S1)NC3=NC=C(Cl)C(C(F)(F)F)=C3
Synonyms :
TAK-580; MLN2480; BUB 024
MDL No. :MFCD22571730
InChI Key :VWMJHAFYPMOMGF-ZCFIWIBFSA-N
Pubchem ID :25161177

Safety of Tovorafenib

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

Related Pathways of Tovorafenib

MAPK

Isoform Comparison

Biological Activity

Target
  • Raf

In Vitro:

Cell Line
Concentration Treated Time Description References
CRAFWT 94.2 nM Evaluate the inhibitory effect of Tovorafenib on CRAFWT PMC10149214
BRAFV600E 495 nM Evaluate the inhibitory effect of Tovorafenib on BRAFV600E PMC10149214
BRAFWT 633 nM Evaluate the inhibitory effect of Tovorafenib on BRAFWT PMC10149214
ARAFSSDD >3000 nM Evaluate the inhibitory effect of Tovorafenib on ARAFSSDD PMC10149214
HEK293 cells 1 µM 10 min Evaluate the effect of SR9009 on a luciferase reporter driven by the Bmal1 promoter PMC5464455
CRAFSSDD 84.5 nM Evaluate the inhibitory effect of Tovorafenib on CRAFSSDD PMC10149214
P53-/- neuroprogenitor cells 1 µM 4 days Evaluate the inhibitory effect of MLN2480 on BRAFV600E and KIAA1549:BRAF-transformed neuroprogenitor cells, showing that MLN2480 effectively inhibits the proliferation of both BRAF mutant cells. PMC5464455

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NCr-NU mice Intracranial tumor model Oral 30 mg/kg Once daily for 9-28 days Evaluate the inhibitory effect of MLN2480 on intracranial tumor growth, showing that MLN2480 significantly inhibits the growth of BRAFV600E and KIAA1549:BRAF-driven tumors and prolongs mouse survival. PMC5464455

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT06381570 Low-grade Glioma EARLY_PHASE1 RECRUITING 2029-03-21 The Hospital for Sick Children... More >>, Toronto, Ontario, M5G 1X8, Canada Less <<
NCT05760586 Low-grade Glioma APPROVED_FOR_MARKETING - -
NCT01425008 Melanoma|Metastatic Melanoma|S... More >>olid Tumor|Neoplasm Less << PHASE1 COMPLETED 2018-10-16 San Francisco, California, Uni... More >>ted States|Denver, Colorado, United States|Augusta, Georgia, United States|Indianapolis, Indiana, United States|New York, New York, United States|Easton, Pennsylvania, United States|Philadelphia, Pennsylvania, United States|San Antonio, Texas, United States|Lakewood, Washington, United States|Bristol, Avon, United Kingdom|Cambridge, Cambridgeshire, United Kingdom|Chelmsford, Essex, United Kingdom|London, Greater London, United Kingdom|Manchester, Greater Manchester, United Kingdom|Oxford, Oxfordshire, United Kingdom|Newcastle upon Tyne, Tyne & Wear, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.88mL

1.98mL

0.99mL

19.75mL

3.95mL

1.98mL

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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