Vemurafenib (PLX4032, RG7204) 化学構造
分子量: 489.92






  • Compare Raf Inhibitors
  • 研究分野
  • Combination Therapy
  • Vemurafenib (PLX4032, RG7204)のメカニズム



製品説明 Vemurafenib (PLX4032, RG7204)新しくて強力な阻害剤で、 B-RAFV600Eに作用すると、IC50 が 31 nMになる。
ターゲット B-RafV600E C-Raf MAP4K5 (KHS1) SRMS ACK1 FGR
IC50 31 nM 48 nM 51 nM 18 nM 19 nM 63 nM [1]
In vitro試験 PLX4032 inhibits B-RAFV600E, C-RAF, as well as wildtype B-RAF, with IC50 of 31 nM, 48 nM and 100 nM, respectively. PLX4032 also inhibits several non-RAF kinases, including ACK1, KHS1, and SRMS, with IC50 of 18 nM to 51 nM. [1] In melanoma cell lines, the inhibitory effect by PLX4032 depends on B-RAF mutational status, because PLX4032 potently inhibits those harboring B-RAF V600 mutants, including V600E, V600D, V600K, and V600R, but not wildtype or other mutants. The IC50 values of PLX4032 on these cells, including MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058, ranges from 20 nM to 1 μM. In these cells, PLX4032 (0.1 μM to 30 μM) also inhibits the phosphorylation of both MEK1/2 and ERK1/2. [2] PLX4032 is highly effective in the treatment of melanoma, for its ability of inhibiting B-RAFV600E. However, PLX4032 displays limited effect in colon cancer patients that also carrying B-RAFV600E oncoprotein. The reason for this is that, in colon cancer cells, B-RAFV600E inhibition by PLX4032 results in a rapid feedback EGFR activation, which compensates for the PLX4032-inhibited cell proliferation. [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
A375 MoLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLiNVAxKM7:TR?= NIfLSHI6PiCq NH3tU2tFVVOR M{fJWWlEPTB;NEegcm0> Mnv2NVg1PThyNUO=
ARO MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYexNFAh|ryP NEXTcII6PiCq NXnwOplvTE2VTx?= MU\JR|UxRTJyNTDuUS=> Mnm1NVg1PThyNUO=
TPCI NHHTN5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fqc|ExOCEQvF2= NELkNWU6PiCq MoHySG1UVw>? M3HKeGlEPTB;MUCuO|ch|ryP MknkNVg1PThyNUO=
A375 MX7BdI9xfG:|aYOgRZN{[Xl? NGDNPG4yOCEQvF2= MV\EUXNQ NHyyOZZRem:vb4Tld{BieG:ydH;0bYMh\GWjdHi= MorDNVg1PThyNUO=
8505C (BRAF V600E/V600E) MmL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWW5OkBp MWjJR|UxRTV5IH7NJC=> NXHKeHlJOjBzNEmxN|Y>
SW1736 (BRAF WT/V600E) NH7pUolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXW5OkBp NGTv[2FKSzVyPUK5JI5O NFPuUHEzODF2OUGzOi=>
BHT101 (BRAF WT/V600E) MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\jOnU6PiCq MU\JR|UxRTl5IH7N NF\QSIUzODF2OUGzOi=>
BCPAP (BRAF WT/V600E) MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XjWVk3KGh? M3vKWWlEPTB;N{igcm0> NYjO[Y5HOjBzNEmxN|Y>
C643 (HRAS G13R)≥ 500 M3K5fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTwPVYhcA>? NXTzb|kxUUN3MDFijcUhPTByIH7N M3P3T|IxOTR7MUO2
CAL62 (KRAS G12R) > 1000 > 1000 NYTnUXY3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXL0fHRyQTZiaB?= MX7JR|UxRiBzMECwJI5O MXWyNFE1QTF|Nh?=
TPC-1 (RET/PTC1) MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXu5OkBp MnHPTWM2OOLLpUGwNFAhdk1? NE\vSJczODF2OUGzOi=>
Calu-6 M2fsb2Z2dmO2aX;uJGF{e2G7 MWCx5qCK|ryP MlfxNUBp NUn1TWhWTE2VTx?= MW\BZ5RqfmG2ZYOgUWVMN0WUSzDpckBk\WyuczD3bZRpKHerbHSteJlx\SCEUlHG NHm2ZpQzODF5OUewOS=>
C4 NWq1NIVkTnWwY4Tpc44hSXO|YYm= MYezJO69VQ>? MYK0PEBp MkHvSG1UVw>? M{DDRmlv[3KnYYPld{Bkd2yuYXflckB{gW62aHXzbZMh[W6mIHTlZ5Jm[XOnczDJUE05KGW6cILld5Nqd25? NGq4N4szPTl6OUWwOi=>
VMM12 MnXvSpVv[3Srb36gRZN{[Xl? MWezJO69VQ>? NUHKenhXPDhiaB?= NVLUVpQ{TE2VTx?= MoLmTY5kemWjc3XzJINwdGyjZ3XuJJN6dnSqZYPpd{BidmRiZHXjdoVie2W|IFnMMVkh\XiycnXzd4lwdg>? NGr2dHEzPTl6OUWwOi=>
UKF-NB-3 (ABCB1) MkTxSpVv[3Srb36gRZN{[Xl? MoK4NU4zPSEEtV2= NW\NdGh6OiCq NWfBN2xrTE2VTx?= M1T0bWVvcGGwY3XzJIFk[3WvdXzheIlwdiCxZjD0bIUh\my3b4Lld4NmdnRiQVLDRlEhe3Wkc4TyZZRmKHKqb3ThcYlv\SBzMkO= MWWyOFc{PTd4Nh?=
UKF-NB-3 NHXPcnpHfW6ldHnvckBCe3OjeR?= MY[xMlI2KML3TR?= MmnvNkBp NYjyfmtkTE2VTx?= NWSyOZBUW2mpbnnmbYNidnSueTDh[oZm[3S|IH;uJIFk[3WvdXzheIlwdiCxZjD0bIUh\my3b4Lld4NmdnRiQVLDRlEhe3Wkc4TyZZRmKHKqb3ThcYlv\SBzMkO= M3vEW|I1PzN3N{[2
A375 (BRAFV600E) MYLGeY5kfGmxbjDBd5NigQ>? MoHMPEBp MX7EUXNQ NYS3dld6UW6lcnXhd4V{KGmwdILhZ4VtdHWuYYKgVm9UKGGwZDDOU{Bt\X[nbIOg M4fhVVI2OzZ|NkS0

... Click to View More Cell Line Experimental Data

In vivo試験 In B-RAFV600E-mutant mice xenograft models, PLX4032 (6 mg/kg–20 mg/kg) inhibits tumor growth. [1] In mice xenograft models of LOX, Colo829, and A375 cells, PLX4032 (12.5 mg/kg–100 mg/kg) inhibits tumor growth and prolongs mice survival. [2]
臨床試験 PLX4032 has recently been approved by US Food and Drug Administration (FDA) for the treatment of advanced metastatic melanoma with a B-RAFV600E mutation.
特集 A novel and potent inhibitor of the B-RAFV600E oncoprotein.

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

RAF kinase activity measurements The kinase activities of wild-type RAF and mutants are determined by measuring phosphorylation of biotinylated-BAD protein. For each enzyme (0.01 ng), 20 μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% (v/v) Tween-20, 50 nM biotin-BAD protein, and 1 mM ATP at room temperature. Reactions are stopped at 5 min with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, 0.3% (w/v) bovine serum albumin (BSA). The stop solution also includes phospho-BAD (Ser112) antibody, streptavidin-coated donor beads, and protein A acceptor beads. The antibody and beads are pre-incubated in stop solution in the dark at room temperature for 30 min. The final dilution of antibody is 1/2000 and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour and then are read on a PerkinElmer AlphaQuest reader. Mutant activities are the average of two different batches of purified protein assayed in duplicate in three different experiments.

細胞アッセイ: [2]

細胞株 MALME-3M, Colo829, Colo38, A375, SK-MEL28, and A2058 cells
濃度 0–10 μM , dissolved in DMSO
反応時間 5 days
実験の流れ Cellular proliferation is evaluated by MTT assay. Briefly, cells are plated in 96-well microtiter plates at a density of 1000 to 5000 cells per well in a volume of 180 μL. PLX4032 is prepared at 10 times the final assay concentration in media containing 1% DMSO. Twenty-four hours after cell plating, 20 μL of the appropriate dilution of PLX4032 are added to plates in duplicate. The plates are assayed for proliferation 6 days after the cells are plated. Percent inhibition is calculated and the IC50 is determined from the regression of a plot of the logarithm of the concentration versus percent inhibition.

動物実験: [2]

動物モデル Mice (athymic nude) xenograft models of LOX, Colo829, and A375 cells
製剤 Formulated as microprecipitated bulk powder (MBP), suspended at the desired concentration in an aqueous vehicle containing 2% Klucel LF, and adjusted to pH 4 with dilute HCl
投薬量 12.5 mg/kg–100 mg/kg
投与方法 Oral gavage twice daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download Vemurafenib (PLX4032, RG7204) SDF
分子量 489.92


CAS No. 918504-65-1
保管 3年-20℃
2年-80℃in solvent
別名 RO5185426
溶解度 (25°C) * In vitro DMSO 97 mg/mL (197.99 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 N-​[3-​[[5-​(4-​chlorophenyl)​-​1H-​pyrrolo[2,​3-​b]​pyridin-​3-​yl]​carbonyl]​-​2,​4-​difluorophenyl]​-1-​propanesulfonamide

文献中の引用 (69)

Frequently Asked Questions

  • Question 1
    How about the half-life of Vemurafenib(S1267)?

    Answer: It was reported that the half-life of the compound is 57 hours.

  • Question 2
    The vemurafenib power, when prepared in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O solutions, form a pellet down the tube?

    Answer: When prepare this kind of vehicle, please dissolve the drug in DMSO clearly first. If it dissolves not readily, please sonicate and warm in the water bath at about 45 degree. Then add PEG and Tween. After they mixed homogeneously, then dilute with water.



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


* 必須

Related Raf 阻害剤

  • LY3009120

    LY03009120 is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.

  • GDC-0994

    GDC-0994 is a potent, orally available ERK1/2 inhibitor. Phase 1.

  • Ulixertinib (BVD-523, VRT752271)

    Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

  • Cobimetinib (GDC-0973, RG7420)

    Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM. Phase 3.

  • Dabrafenib (GSK2118436)

    Dabrafenib(GSK2118436)は、B-Rafの強力なATP競争的阻害剤で、 B-Raf、 B-RafV600E 、c-Rafに作用する時、 IC50 がそれぞれ 3.2 nM、 0.8 nM 、 5.0 nMです。

  • Sorafenib

    Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.

  • Sorafenib Tosylate

    Sorafenib Tosylateは一種の多種キナーゼ阻害剤です。Sorafenib Tosylateは無細胞試験でRaf-1、B-RafとVEGFR-2に作用する時のIC50値が6 nM、22 nMと90 nMにそれぞれ分かれます。

  • PLX-4720

    PLX-4720は、B-Raf(V600E)とc-Raf-1(Y340D/Y341D)の「実行中の」形の強力で選択的な阻害剤で、IC50 がそれぞれ 13 nM と 6.7 nMです。

  • TAK-632

    TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf, respectively, showing less or no inhibition against other tested kinases.


Tags: Vemurafenib (PLX4032, RG7204)を買う | Vemurafenib (PLX4032, RG7204)供給者 | Vemurafenib (PLX4032, RG7204)を購入する | Vemurafenib (PLX4032, RG7204)費用 | Vemurafenib (PLX4032, RG7204)生産者 | オーダーVemurafenib (PLX4032, RG7204) | Vemurafenib (PLX4032, RG7204)代理店
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID