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PLX8394

Catalog No. T3579 CAS 1393466-87-9

PLX8394 is an orally active inhibitor of serine/threonine-protein kinase B-Raf (BRAF) protein. PLX8394 can selectively bind to and inhibit the activity of both wild-type and mutated forms of BRAF, then inhibit the proliferation of tumor cells which express mutated forms of BRAF. PLX8394 appears to be effective against tumors that express multiple mutated forms of the kinase and may be an effective therapeutic agent for tumors that are resistant to other BRAF inhibitor therapies that are specific for the BRAF V600E mutant.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PLX8394, CAS 1393466-87-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 44.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 91.00
10 mg	In stock	$ 143.00
25 mg	In stock	$ 258.00
50 mg	In stock	$ 383.00
100 mg	In stock	$ 559.00
1 mL * 10 mM (in DMSO)	In stock	$ 123.00

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Purity: 100%

Purity: 98.22%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PLX8394 is an orally active inhibitor of serine/threonine-protein kinase B-Raf (BRAF) protein. PLX8394 can selectively bind to and inhibit the activity of both wild-type and mutated forms of BRAF, then inhibit the proliferation of tumor cells which express mutated forms of BRAF. PLX8394 appears to be effective against tumors that express multiple mutated forms of the kinase and may be an effective therapeutic agent for tumors that are resistant to other BRAF inhibitor therapies that are specific for the BRAF V600E mutant.
Targets&IC50	BRAF:14 nM, Raf:23 nM, B-Raf (V600E):3.8 nM
In vitro	PLX8394 (>25 nM) effectively inhibits phosphorylation of ERK1/2 in PRT 3 and PRT 4 cells and in addition to parental cells at 10 nM. PLX8394 effectively reduces phosphorylation of retinoblastoma protein, cyclin D3/D1, and expression of cyclin A2 in parental cells and PRT 3/4 cells. PLX8394 inhibits ERK1/2 phosphorylation and the growth of vemurafenib-resistant cells harboring either a BRAF V600K/L505H double mutation or a 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	In mice H1755 xenograft tumors, PLX8394 (150 mg/kg/day) substantially suppresses tumor growth, tumor cell proliferation and MAPK pathway signaling without overt toxicity. PLX8394 combines with erlotinib yields plasma erlotinib concentrations of >1 μM[2].
Cell Research	Dissolvent: DMSO. 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 Research	PLX8394 is dissolved in PEG 400 [20% (v/v)], TPGS [5% (v/v)], and water [75% (v/v)].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 (p.o.) is given at a dose of 150 mg/kg/d.

Molecular Weight	542.53
Formula	C25H21F3N6O3S
CAS No.	1393466-87-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (92.16 mM)

References and Literature

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. PreClinicalal 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Apoptosis Compound Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library

Related Products

Related compounds with same targets

Encorafenib SOS1-IN-11 Sorafenib KG5 CCT241161 Plx-4032 GSK2008607 LUT014

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Keywords

PLX8394 1393466-87-9 MAPK Raf PLX-8394 PLX 8394 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.