PLX8394

Modify Date: 2024-01-08 18:27:16

PLX8394 Structure
PLX8394 structure
Common Name PLX8394
CAS Number 1393466-87-9 Molecular Weight 542.533
Density 1.6±0.1 g/cm3 Boiling Point 786.8±70.0 °C at 760 mmHg
Molecular Formula C25H21F3N6O3S Melting Point N/A
MSDS N/A Flash Point 429.6±35.7 °C

 Use of PLX8394


PLX8394 is a potent and selective Raf inhibitor, with an IC50 of appr 5 nM for BRAFV600E.

 Names

Name plx8394
Synonym More Synonyms

 PLX8394 Biological Activity

Description PLX8394 is a potent and selective Raf inhibitor, with an IC50 of appr 5 nM for BRAFV600E.
Related Catalog
Target

BRafV600E:5 nM (IC50)

In Vitro PLX8394 potently inhibits phosphorylation of ERK1/2 in PRT #3 and PRT #4 cells at >25 nM and in addition to parental cells at 10 nM. PLX8394 effectively reduces cyclin D3 and cyclin D1, phosphorylation of retinoblastoma protein, and expression of cyclin A2 in parental cells and PRT #3 and PRT #4 cells. PLX8394 inhibits ERK1/2 phosphorylation and the growth of vemurafenib-resistant cells harboring either a BRAF V600K/L505H double mutation or an transposon-induced, N-terminal truncated form of BRAF[1]. PLX8394 significantly impairs tumor cell growth and suppresses MAPK signaling in LA cell lines expressing either endogenous V600E or non-V600 mutant forms of BRAF[2].
In Vivo PLX8394 (150 mg/kg/d) substantially suppresses tumor growth, MAPK pathway signaling and tumor cell proliferation in these H1755 xenograft tumors without overt toxicity in mice. PLX8394 combines with erlotinib yields plasma erlotinib concentrations of >1 μM[2].
Cell Assay For MTT assays, 2×103 cells are seeded in triplicate in 96 wells in their regular culture medium (containing PLX4720 for PRT lines). Next day, cells are washed twice with PBS and then the medium is replenished containing the indicated RAF inhibitor. Medium is changed 48 hours later and after a further 48 hours, 10 μL of 5 mg/mL MTT reagent is added to wells, and incubated for three hours. Formazan crystals are then solubilized overnight with a 1:10 dilution of 0.1 M glycine (pH 10.5) in DMSO. Wells are then analyzed at 450 nM in a Multiskan® Spectrum spectrophotometer. Results depicted are normalized to DMSO conditions and are a composite of three independent experiments. Error bars shown are representative of the standard error of mean (SEM).
Animal Admin H1755 tumor xenografts are generated by injection of 5×106 cells in a 50/50 mixture for matrigel and PBS into 6- to 8-wk-old female NOD/SCID mice. Mice are randomized to treatment groups once tumors reach an average size of 150 mm3. H1755 cells are s.c. implanted and allowed to grow to appr 200 mm3 (4 wk after implantation). Mice are then treated with vehicle, vemurafenib, or PLX8394 for 15 d. The vehicle for daily oral gavage is PEG 400 [20% (vol/vol)], tocopheryl polyethylene glycol succinate (TPGS) [5% (vol/vol)], water [75% (vol/vol)]. PLX8394 is dissolved in PEG 400 [20% (vol/vol)], TPGS [5% (vol/vol)], and water [75% (vol/vol)] and vortexed continuously throughout the dosing period. PLX8394 is given daily by oral gavage at a dose of 150 mg/kg/d.
References

[1]. Basile KJ, et al. Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors. Pigment Cell Melanoma Res. 2014 May;27(3):479-484.

[2]. Okimoto RA, et al. Preclinical efficacy of a RAF inhibitor that evades paradoxical MAPK pathway activation in protein kinase BRAF-mutant lung cancer. Proc Natl Acad Sci U S A. 2016 Nov 22;113(47):13456-13461

 Chemical & Physical Properties

Density 1.6±0.1 g/cm3
Boiling Point 786.8±70.0 °C at 760 mmHg
Molecular Formula C25H21F3N6O3S
Molecular Weight 542.533
Flash Point 429.6±35.7 °C
Exact Mass 542.134766
LogP 0.97
Vapour Pressure 0.0±2.7 mmHg at 25°C
Index of Refraction 1.703
Storage condition -20℃

 Synonyms

1-Pyrrolidinesulfonamide, N-[3-[[5-(2-cyclopropyl-5-pyrimidinyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-3-fluoro-, (3R)-
(3R)-N-(3-{[5-(2-Cyclopropyl-5-pyrimidinyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl}-2,4-difluorophenyl)-3-fluoro-1-pyrrolidinesulfonamide
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: PLX8394
  • Price: $800.0/100mg $1600.0/250mg $3200.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

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Price: $129/10mM*1mLinDMSO

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