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Chemical Structure| 1446113-23-0 Chemical Structure| 1446113-23-0

Structure of Belvarafenib
CAS No.: 1446113-23-0

Chemical Structure| 1446113-23-0

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Belvarafenib is a pan-RAF inhibitor, with IC50 values of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFV600E and C-RAF, respectively.

Synonyms: HM95573; GDC-5573; RG6185

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Product Details of Belvarafenib

CAS No. :1446113-23-0
Formula : C23H16ClFN6OS
M.W : 478.93
SMILES Code : O=C(C1=CSC2=C(N)N=CN=C21)NC3=C(C)C=CC4=C3C=CN=C4NC5=CC=CC(Cl)=C5F
Synonyms :
HM95573; GDC-5573; RG6185
MDL No. :MFCD31731098
InChI Key :KVCQTKNUUQOELD-UHFFFAOYSA-N
Pubchem ID :89655386

Safety of Belvarafenib

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 Belvarafenib

MAPK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293T cells 1 μM 4 hours Belvarafenib significantly promoted BRAF/RAF1 heterodimer formation PMC10265822
SK-MEL-30 1 to 0.002 µM 120 hours Evaluate the effect of Belvarafenib and Cobimetinib on NRAS mutant cells, showing synergistic effects in the NRAS mutant context. PMC11353013
SK-MEL-2 1 to 0.002 µM 120 hours Evaluate the effect of Belvarafenib and Cobimetinib on NRAS mutant cells, showing synergistic effects in the NRAS mutant context. PMC11353013
MEL-JUSO 1 to 0.002 µM 120 hours Evaluate the effect of Belvarafenib and Cobimetinib on NRAS mutant cells, showing synergistic effects in the NRAS mutant context. PMC11353013
IPC-298 1 to 0.002 µM 120 hours Evaluate the effect of Belvarafenib and Cobimetinib on NRAS Q61L mutant cells, showing synergistic effects in the NRAS mutant context. PMC11353013
A375 1 to 0.002 µM 120 hours Evaluate the effect of Belvarafenib and Cobimetinib on BRAF V600E mutant cells, showing additive effects in the BRAF mutant context. PMC11353013
IPC-298 cells 10 µM 90 days Investigated the transcriptomic response of melanoma cells to Belvarafenib, discovering a rare resistant cell population (0.12%) PMC11499997

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NCR.nude mice IPC-298 xenograft model Oral gavage 15 mg/kg or 30 mg/kg Once daily for 21 days Evaluate the antitumor effect of Belvarafenib and Cobimetinib in NRAS Q61L mutant xenograft model, showing synergistic effects in combination therapy. PMC11353013

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03118817 Solid Tumor PHASE1 COMPLETED 2020-02-04 Korea, Republic of, Chungcheon... More >>gbuk-do, Cheongju, Chungcheongbuk-do, 28644, Korea, Republic of|Korea, Republic of, Gyeonggi-do, Seongnam, Gyeonggi-do, 13620, Korea, Republic of|Korea, Republic of, Gyeongsangbuk-do, Daegu, Gyeongsangbuk-do, 41404, Korea, Republic of|Korea, Republic of, Seoul, Seoul, 03722, Korea, Republic of|Korea, Republic of, Seoul, Seoul, 05505, Korea, Republic of|Korea, Republic of, Seoul, Seoul, 06351, Korea, Republic of|Korea, Republic of, Seoul, Seoul, 07061, Korea, Republic of Less <<
NCT02405065 Neoplasms PHASE1 COMPLETED 2018-05-16 Hanmi Clinical, Seoul, 05545, ... More >>Korea, Republic of Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.44mL

2.09mL

1.04mL

20.88mL

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

References

 

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