Home Cart Sign in  
Chemical Structure| 918505-84-7 Chemical Structure| 918505-84-7

Structure of PLX4720
CAS No.: 918505-84-7

Chemical Structure| 918505-84-7

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

PLX 4720 is a potent and selective inhibitor of B-RafV600E (IC50=13 nM) and c-Raf-1Y340D/Y341D (IC50=6.7 nM), whth a 10-fold selectivity for B-RafV600E than wild-type B-Raf.

Synonyms: PLX-4720

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of PLX4720

CAS No. :918505-84-7
Formula : C17H14ClF2N3O3S
M.W : 413.83
SMILES Code : CCCS(=O)(NC1=CC=C(F)C(C(C2=CNC3=NC=C(Cl)C=C32)=O)=C1F)=O
Synonyms :
PLX-4720
MDL No. :MFCD14635203
InChI Key :YZDJQTHVDDOVHR-UHFFFAOYSA-N
Pubchem ID :24180719

Safety of PLX4720

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

Related Pathways of PLX4720

MAPK

Isoform Comparison

Biological Activity

Target
  • B-Raf

    B-Raf, IC50:160 nM

    B-Raf (V600E), IC50:13 nM

  • C-Raf/Raf-1

    C-Raf-1 (Y340D/Y341D), IC50:6.7 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
A375 0.66 μM 24 h Generate sub-lines with acquired resistance to PLX4720 PMC6856071
NAE cells 1 µM, 3 µM, 10 µM, 30 µM 48 h To evaluate the synergistic effect of PLX4720 with Nt-3, results showed significant synergism in NAE cells PMC3777641
A375 cells 2 µM 24 h To evaluate the effect of PLX4720 on A375 cells, results showed decreased levels of pERK and cyclinD1 PMC3777641
WM239 cells 2 µM 24 h To evaluate the effect of PLX4720 on WM239 cells, results showed decreased levels of pERK and cyclinD1 PMC3777641
LM-MEL-33, LM-MEL-64, LM-MEL-70 1 μM 0, 3, 7, 11, 17, 35, and 70 days To evaluate the effect of PLX4720 on melanoma cell lines harboring BRAF activating mutations and observe phenotypic changes post-treatment. Results showed significant phenotypic changes after 3 days of drug treatment, followed by stabilization at 11, 17, and 35 days. Chronic exposure to PLX4720 resulted in similar cell phenotypes, indicating the selection effect of drug resistance. PMC5902511
A375 cells 5 µM 8-72 h To test the protective effect of TNF α on PLX4720-induced apoptosis, results showed that TNF α significantly inhibited the activation of caspase 3, 8, and 9 induced by PLX4720. PMC4466037
M238 cells 5 µM 8-72 h To test the protective effect of TNF α on PLX4720-induced apoptosis, results showed that TNF α significantly inhibited the activation of caspase 3, 8, and 9 induced by PLX4720. PMC4466037
M229 cells 5 µM 8-72 h To test the protective effect of TNF α on PLX4720-induced apoptosis, results showed that TNF α significantly inhibited the activation of caspase 3, 8, and 9 induced by PLX4720. PMC4466037

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Apc Min +/− mice Oral 60 mg/kg Daily for 28 days To evaluate the effect of PLX4720 on intestinal polyp formation in Apc Min +/? mice, the results showed that PLX4720 significantly increased the number of intestinal polyps in mice. PMC4668213
Mice BrafV600E-mutant melanoma model Oral 417mg/kg 4 days PLX4720 was used to inhibit BRAF mutation, delaying tumor growth, but alone it failed to prevent tumor relapse. PMC4980762
mice Braf/Nf1 mutant melanoma allograft model intraperitoneal injection 2.5mg/kg daily for 7 days To evaluate the therapeutic effect of PLX4720 on Braf/Nf1 mutant melanomas, results showed these tumors were relatively insensitive to PLX4720 PMC3595355
Nude mice A375 xenograft model Intraperitoneal injection 50 mg/kg Once daily for two weeks To evaluate the inhibitory effect of PLX4720 on tumor growth, results showed PLX4720 significantly suppressed tumor growth PMC3777641
nude mice WM35 and WM983B xenograft model oral 417 mg/kg once daily for 21 days To study the effect of ROR1 knockdown on the response to PLX4720 treatment, results showed that ROR1 knockdown significantly decreased sensitivity to PLX4720 PMC3918498
nude mice A375TR xenograft model oral 90 mg/kg once daily for 28 days To test the anti-tumor effect of PLX4720 combined with NFκB pathway inhibitors, results showed that combination therapy significantly inhibited tumor growth. PMC4466037

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.08mL

2.42mL

1.21mL

24.16mL

4.83mL

2.42mL

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
 

Historical Records

Categories