Testing Data
(PLX4720, a 7-azaindole derivative that inhibits B-RafV600E with an IC50 of 13 nM, defines a class of kinase inhibitor with marked selectivity in both biochemical and cellular assays. PLX4720 preferentially inhibits the active B-RafV600E kinase compared with a broad spectrum of other kinases (IC50:B-Raf=160 nM, BRK=130 nM, other kinases >1000nM), and potent cytotoxic effects are also exclusive to cells bearing the V600E allele (GI5010 uM). [1]Consistent with the high degree of selectivity, ERK phosphorylation is potently inhibited by PLX4720 in B-RafV600E -bearing tumor cell lines but not in cells lacking oncogenic B-Raf. [1]In B-RafV600E -dependent tumor xenograft models, orally dosed PLX4720 causes significant tumor growth delays, including tumor regressions, without evidence of toxicity. [1])
PLX-4720, inhibitor
PLX-4720
Purity
>99%
Synonyms
PLX-4720; inhibitor
Purity/Purification
>99%
Solubility
DMSO >=83mg/mL - Water <1mg/mL - Ethanol <1mg/mL
Formula
C17H14ClF2N3O3S
CAS Number
918505-84-7
Preparation and Storage
Store at-20 degree C 2 years.
Testing Data
(PLX4720, a 7-azaindole derivative that inhibits B-RafV600E with an IC50 of 13 nM, defines a class of kinase inhibitor with marked selectivity in both biochemical and cellular assays. PLX4720 preferentially inhibits the active B-RafV600E kinase compared with a broad spectrum of other kinases (IC50:B-Raf=160 nM, BRK=130 nM, other kinases >1000nM), and potent cytotoxic effects are also exclusive to cells bearing the V600E allele (GI5010 uM). [1]Consistent with the high degree of selectivity, ERK phosphorylation is potently inhibited by PLX4720 in B-RafV600E -bearing tumor cell lines but not in cells lacking oncogenic B-Raf. [1]In B-RafV600E -dependent tumor xenograft models, orally dosed PLX4720 causes significant tumor growth delays, including tumor regressions, without evidence of toxicity. [1])
Testing Data
(PLX4720, a 7-azaindole derivative that inhibits B-RafV600E with an IC50 of 13 nM, defines a class of kinase inhibitor with marked selectivity in both biochemical and cellular assays. PLX4720 preferentially inhibits the active B-RafV600E kinase compared with a broad spectrum of other kinases (IC50:B-Raf=160 nM, BRK=130 nM, other kinases >1000nM), and potent cytotoxic effects are also exclusive to cells bearing the V600E allele (GI5010 uM). [1]Consistent with the high degree of selectivity, ERK phosphorylation is potently inhibited by PLX4720 in B-RafV600E -bearing tumor cell lines but not in cells lacking oncogenic B-Raf. [1]In B-RafV600E -dependent tumor xenograft models, orally dosed PLX4720 causes significant tumor growth delays, including tumor regressions, without evidence of toxicity. [1])
Related Product Information for PLX-4720, inhibitor
PLX4720, a 7-azaindole derivative that inhibits B-RafV600E with an IC50 of 13 nM, defines a class of kinase inhibitor with marked selectivity in both biochemical and cellular assays. PLX4720 preferentially inhibits the active B-RafV600E kinase compared with a broad spectrum of other kinases (IC50:B-Raf=160 nM, BRK=130 nM, other kinases >1000nM), and potent cytotoxic effects are also exclusive to cells bearing the V600E allele (GI50<1.7 muM, while other wild cell GI50>10muM). [1] Consistent with the high degree of selectivity, ERK phosphorylation is potently inhibited by PLX4720 in B-RafV600E-bearing tumor cell lines but not in cells lacking oncogenic B-Raf. [1] In B-RafV600E-dependent tumor xenograft models, orally dosed PLX4720 causes signi?cant tumor growth delays, including tumor regressions, without evidence of toxicity. [1]
Product Categories/Family for PLX-4720, inhibitor
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Product Notes
The PLX-4720 (Catalog #AAA8506422) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "PLX-4720, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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