PLX-4720

製品コード：S1152 純度：99.98%

PLX4720 is a potent and selective inhibitor of B-Raf^V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

CAS No. 918505-84-7

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
25mg	JPY 40500	国内在庫あり
100mg	JPY 100500	国内在庫あり
1g	JPY 220500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（189）

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

PLX-4720と併用されることが多い化合物

Dactolisib (BEZ235)

PLX-4720 and Dactolisib treatment decreases both pERK and pAKT levels in Colo-205 xenografts.

Schulte ML, et al. Mol Imaging Biol. 2017 Jun;19(3):421-428.

Navitoclax (ABT-263)

PLX-4720 and Navitoclax can enhance the clinical efficacy of BRAF inhibitors.

Frederick DT, et al. Cancer Res (2013) 73 (8_Supplement): 1724.

NMS-E973

PLX-4720 and NMS-E973 show a synergic antiproliferative activity in A375 melanoma cells.

Fogliatto G, et al. Clin Cancer Res. 2013 Jul 1;19(13):3520-32.

SB431542

PLX-4720 and SB431542 cotreatment abolish the increase in cell growth caused by low-dose PLX-4720 in Colo829 and A375(M2) cells.

Spender LC, et al. Oncotarget. 2016 Dec 13; 7(50): 81995–82012.

PLX-4720関連製品

関連ターゲット	C-Raf/Raf-1 B-Raf A-raf	もっと見る
関連製品	LY3009120 AZ 628 GDC-0879 SB590885 TAK-632 RAF265 (CHIR-265) GW5074 Avutometinib PLX7904 Plixorafenib (PLX8394) ZM 336372 Naporafenib (LXH254) Lifirafenib (BGB-283) Agerafenib (CEP-32496) Tovorafenib (MLN2480) Belvarafenib B-Raf inhibitor 1 (Compound 13) dihydrochloride RAF709 CCT196969	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library MAPK Inhibitor Library Cell Cycle compound library TGF-beta/Smad compound library Anti-alzheimer Disease Compound Library	もっと見る

シグナル伝達経路

Rafシグナル伝達経路

Raf阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
A375	Cytotoxicity assay	72 hrs	Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.5 μM.	29461827
SK-LU-1	Growth Inhibition Assay		IC50=12.2655 μM	SANGER
A3-KAW	Growth Inhibition Assay		IC50=11.7178 μM	SANGER
SK-HEP-1	Growth Inhibition Assay		IC50=11.3527 μM	SANGER
KNS-62	Growth Inhibition Assay		IC50=11.2404 μM	SANGER
NOS-1	Growth Inhibition Assay		IC50=10.8472 μM	SANGER
SK-MEL-24	Growth Inhibition Assay		IC50=10.8274 μM	SANGER
LXF-289	Growth Inhibition Assay		IC50=10.458 μM	SANGER
A431	Growth Inhibition Assay		IC50=10.4212 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay		IC50=10.0149 μM	SANGER
RS4-11	Growth Inhibition Assay		IC50=9.6048 μM	SANGER
JVM-3	Growth Inhibition Assay		IC50=9.56999 μM	SANGER
KY821	Growth Inhibition Assay		IC50=9.05178 μM	SANGER
GCT	Growth Inhibition Assay		IC50=8.75314 μM	SANGER
SW982	Growth Inhibition Assay		IC50=8.41516 μM	SANGER
HSC-3	Growth Inhibition Assay		IC50=8.07068 μM	SANGER
COLO-741	Growth Inhibition Assay		IC50=8.01679 μM	SANGER
LB2241-RCC	Growth Inhibition Assay		IC50=7.36907 μM	SANGER
BCPAP	Growth Inhibition Assay		IC50=7.21764 μM	SANGER
HCC1806	Growth Inhibition Assay		IC50=6.81931 μM	SANGER
CAL-72	Growth Inhibition Assay		IC50=6.45423 μM	SANGER
H4	Growth Inhibition Assay		IC50=6.22493 μM	SANGER
NB7	Growth Inhibition Assay		IC50=6.21373 μM	SANGER
8-MG-BA	Growth Inhibition Assay		IC50=6.18129 μM	SANGER
ES5	Growth Inhibition Assay		IC50=6.14924 μM	SANGER
HT-1080	Growth Inhibition Assay		IC50=6.10946 μM	SANGER
TI-73	Growth Inhibition Assay		IC50=6.00902 μM	SANGER
CHL-1	Growth Inhibition Assay		IC50=5.97603 μM	SANGER
RPMI-7951	Growth Inhibition Assay		IC50=5.80283 μM	SANGER
8305C	Growth Inhibition Assay		IC50=5.1873 μM	SANGER
KG-1	Growth Inhibition Assay		IC50=4.73908 μM	SANGER
A2058	Growth Inhibition Assay		IC50=4.72164 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay		IC50=4.53325 μM	SANGER
NB13	Growth Inhibition Assay		IC50=4.49179 μM	SANGER
CP66-MEL	Growth Inhibition Assay		IC50=4.15927 μM	SANGER
697	Growth Inhibition Assay		IC50=3.55266 μM	SANGER
CTB-1	Growth Inhibition Assay		IC50=3.40176 μM	SANGER
NCI-H358	Growth Inhibition Assay		IC50=2.92232 μM	SANGER
HuO-3N1	Growth Inhibition Assay		IC50=2.87946 μM	SANGER
PA-1	Growth Inhibition Assay		IC50=2.72673 μM	SANGER
KP-4	Growth Inhibition Assay		IC50=2.30787 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay		IC50=2.11969 μM	SANGER
KARPAS-45	Growth Inhibition Assay		IC50=2.04978 μM	SANGER
HTC-C3	Growth Inhibition Assay		IC50=1.66294 μM	SANGER
NCI-H209	Growth Inhibition Assay		IC50=1.6086 μM	SANGER
SK-MEL-30	Growth Inhibition Assay		IC50=1.33386 μM	SANGER
MZ7-mel	Growth Inhibition Assay		IC50=1.14963 μM	SANGER
COLO-679	Growth Inhibition Assay		IC50=1.10464 μM	SANGER
SK-MEL-28	Growth Inhibition Assay		IC50=1.04569 μM	SANGER
WM-115	Growth Inhibition Assay		IC50=0.88692 μM	SANGER
HCC2218	Growth Inhibition Assay		IC50=0.87844 μM	SANGER
RVH-421	Growth Inhibition Assay		IC50=0.86796 μM	SANGER
BV-173	Growth Inhibition Assay		IC50=0.79644 μM	SANGER
K5	Growth Inhibition Assay		IC50=0.76148 μM	SANGER
BHT-101	Growth Inhibition Assay		IC50=0.70702 μM	SANGER
MMAC-SF	Growth Inhibition Assay		IC50=0.68614 μM	SANGER
A375	Growth Inhibition Assay		IC50=0.67359 μM	SANGER
SK-MEL-3	Growth Inhibition Assay		IC50=0.51568 μM	SANGER
SH-4	Growth Inhibition Assay		IC50=0.41422 μM	SANGER
MEL-HO	Growth Inhibition Assay		IC50=0.41179 μM	SANGER
COLO-829	Growth Inhibition Assay		IC50=0.38968 μM	SANGER
ACN	Growth Inhibition Assay		IC50=0.38477 μM	SANGER
HT-144	Growth Inhibition Assay		IC50=0.36329 μM	SANGER
G-361	Growth Inhibition Assay		IC50=0.34637 μM	SANGER
A101D	Growth Inhibition Assay		IC50=0.32589 μM	SANGER
CP50-MEL-B	Growth Inhibition Assay		IC50=0.29784 μM	SANGER
M14	Growth Inhibition Assay		IC50=0.21757 μM	SANGER
C32	Growth Inhibition Assay		IC50=0.15131 μM	SANGER
EoL-1-cell	Growth Inhibition Assay		IC50=0.14166 μM	SANGER
DU-4475	Growth Inhibition Assay		IC50=0.07457 μM	SANGER
TYK-nu	Growth Inhibition Assay		IC50=12.3932 μM	SANGER
NMC-G1	Growth Inhibition Assay		IC50=12.6062 μM	SANGER
BB65-RCC	Growth Inhibition Assay		IC50=12.7169 μM	SANGER
QIMR-WIL	Growth Inhibition Assay		IC50=12.8833 μM	SANGER
D-566MG	Growth Inhibition Assay		IC50=13.9576 μM	SANGER
KYSE-140	Growth Inhibition Assay		IC50=14.0753 μM	SANGER
SCC-4	Growth Inhibition Assay		IC50=14.3359 μM	SANGER
U251	Growth Inhibition Assay		IC50=14.8492 μM	SANGER
D-542MG	Growth Inhibition Assay		IC50=14.9222 μM	SANGER
LAMA-84	Growth Inhibition Assay		IC50=14.9932 μM	SANGER
NCI-H720	Growth Inhibition Assay		IC50=15.2684 μM	SANGER
DEL	Growth Inhibition Assay		IC50=15.4293 μM	SANGER
SBC-1	Growth Inhibition Assay		IC50=15.4305 μM	SANGER
ECC10	Growth Inhibition Assay		IC50=15.4458 μM	SANGER
Daoy	Growth Inhibition Assay		IC50=15.7616 μM	SANGER
SCH	Growth Inhibition Assay		IC50=15.7835 μM	SANGER
MZ2-MEL	Growth Inhibition Assay		IC50=16.0646 μM	SANGER
CAL-12T	Growth Inhibition Assay		IC50=16.4862 μM	SANGER
KE-37	Growth Inhibition Assay		IC50=16.8107 μM	SANGER
LS-411N	Growth Inhibition Assay		IC50=17.118 μM	SANGER
NCI-H2228	Growth Inhibition Assay		IC50=17.3071 μM	SANGER
SK-MEL-2	Growth Inhibition Assay		IC50=17.4965 μM	SANGER
HN	Growth Inhibition Assay		IC50=17.7248 μM	SANGER
NCI-H1648	Growth Inhibition Assay		IC50=17.818 μM	SANGER
IA-LM	Growth Inhibition Assay		IC50=18.3172 μM	SANGER
EW-13	Growth Inhibition Assay		IC50=18.5708 μM	SANGER
YKG-1	Growth Inhibition Assay		IC50=19.5711 μM	SANGER
KNS-81-FD	Growth Inhibition Assay		IC50=19.5858 μM	SANGER
23132-87	Growth Inhibition Assay		IC50=19.7642 μM	SANGER
NUGC-3	Growth Inhibition Assay		IC50=19.9887 μM	SANGER
5637	Growth Inhibition Assay		IC50=20.0478 μM	SANGER
NCI-H1755	Growth Inhibition Assay		IC50=20.4764 μM	SANGER
RH-18	Growth Inhibition Assay		IC50=20.5748 μM	SANGER
RXF393	Growth Inhibition Assay		IC50=20.6756 μM	SANGER
LU-134-A	Growth Inhibition Assay		IC50=20.7056 μM	SANGER
TE-12	Growth Inhibition Assay		IC50=20.7201 μM	SANGER
MOLT-4	Growth Inhibition Assay		IC50=21.1915 μM	SANGER
IGR-1	Growth Inhibition Assay		IC50=21.3796 μM	SANGER
HOP-92	Growth Inhibition Assay		IC50=21.4987 μM	SANGER
SK-MES-1	Growth Inhibition Assay		IC50=21.7381 μM	SANGER
LU-65	Growth Inhibition Assay		IC50=21.8624 μM	SANGER
MS-1	Growth Inhibition Assay		IC50=22.1203 μM	SANGER
LoVo	Growth Inhibition Assay		IC50=22.244 μM	SANGER
A704	Growth Inhibition Assay		IC50=22.5155 μM	SANGER
HT-1376	Growth Inhibition Assay		IC50=22.6059 μM	SANGER
IST-MEL1	Growth Inhibition Assay		IC50=22.6751 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay		IC50=22.7366 μM	SANGER
T47D	Growth Inhibition Assay		IC50=22.7979 μM	SANGER
HT-1197	Growth Inhibition Assay		IC50=23.0817 μM	SANGER
LB2518-MEL	Growth Inhibition Assay		IC50=23.6412 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay		IC50=24.7595 μM	SANGER
SK-NEP-1	Growth Inhibition Assay		IC50=24.8744 μM	SANGER
NCI-H526	Growth Inhibition Assay		IC50=25.0023 μM	SANGER
IST-SL1	Growth Inhibition Assay		IC50=25.2751 μM	SANGER
HH	Growth Inhibition Assay		IC50=25.3192 μM	SANGER
NCI-H82	Growth Inhibition Assay		IC50=25.938 μM	SANGER
SNU-449	Growth Inhibition Assay		IC50=27.2018 μM	SANGER
COR-L23	Growth Inhibition Assay		IC50=27.2813 μM	SANGER
LOXIMVI	Growth Inhibition Assay		IC50=27.368 μM	SANGER
GR-ST	Growth Inhibition Assay		IC50=27.6706 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay		IC50=27.944 μM	SANGER
ALL-PO	Growth Inhibition Assay		IC50=28.1604 μM	SANGER
ML-2	Growth Inhibition Assay		IC50=28.2814 μM	SANGER
HOP-62	Growth Inhibition Assay		IC50=28.713 μM	SANGER
EGI-1	Growth Inhibition Assay		IC50=28.8845 μM	SANGER
TCCSUP	Growth Inhibition Assay		IC50=28.9272 μM	SANGER
LB996-RCC	Growth Inhibition Assay		IC50=29.5682 μM	SANGER
LCLC-97TM1	Growth Inhibition Assay		IC50=32.1964 μM	SANGER
NCI-H1304	Growth Inhibition Assay		IC50=32.3301 μM	SANGER
KP-N-YS	Growth Inhibition Assay		IC50=32.5973 μM	SANGER
NCI-H1770	Growth Inhibition Assay		IC50=33.1648 μM	SANGER
EM-2	Growth Inhibition Assay		IC50=33.6504 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay		IC50=33.7236 μM	SANGER
ACHN	Growth Inhibition Assay		IC50=33.8385 μM	SANGER
MN-60	Growth Inhibition Assay		IC50=33.8544 μM	SANGER
EW-18	Growth Inhibition Assay		IC50=33.8971 μM	SANGER
KGN	Growth Inhibition Assay		IC50=35.7292 μM	SANGER
U031	Growth Inhibition Assay		IC50=35.8132 μM	SANGER
HMV-II	Growth Inhibition Assay		IC50=36.0774 μM	SANGER
L-363	Growth Inhibition Assay		IC50=37.6455 μM	SANGER
NCI-H1155	Growth Inhibition Assay		IC50=38.0015 μM	SANGER
NCI-H1793	Growth Inhibition Assay		IC50=38.1026 μM	SANGER
P30-OHK	Growth Inhibition Assay		IC50=38.1332 μM	SANGER
AN3-CA	Growth Inhibition Assay		IC50=38.1615 μM	SANGER
UACC-257	Growth Inhibition Assay		IC50=38.79 μM	SANGER
MCF7	Growth Inhibition Assay		IC50=39.8629 μM	SANGER
KP-N-YN	Growth Inhibition Assay		IC50=40.4285 μM	SANGER
T98G	Growth Inhibition Assay		IC50=40.4957 μM	SANGER
HGC-27	Growth Inhibition Assay		IC50=43.274 μM	SANGER
NCI-H1092	Growth Inhibition Assay		IC50=43.2895 μM	SANGER
KARPAS-299	Growth Inhibition Assay		IC50=43.3071 μM	SANGER
LB1047-RCC	Growth Inhibition Assay		IC50=44.9959 μM	SANGER
786-0	Growth Inhibition Assay		IC50=45.65 μM	SANGER
HCC2157	Growth Inhibition Assay		IC50=46.0359 μM	SANGER
NY	Growth Inhibition Assay		IC50=46.1778 μM	SANGER
EFM-19	Growth Inhibition Assay		IC50=46.7533 μM	SANGER
EW-16	Growth Inhibition Assay		IC50=46.7806 μM	SANGER
UM-UC-3	Growth Inhibition Assay		IC50=46.8059 μM	SANGER
HT-29	Growth Inhibition Assay		IC50=47.8792 μM	SANGER
LN-405	Growth Inhibition Assay		IC50=48.0827 μM	SANGER
NCI-H727	Growth Inhibition Assay		IC50=48.7726 μM	SANGER
D-502MG	Growth Inhibition Assay		IC50=48.9676 μM	SANGER
GMS-10	Growth Inhibition Assay		IC50=49.2974 μM	SANGER
MEL-JUSO	Growth Inhibition Assay		IC50=49.347 μM	SANGER
insect cells	Function assay		Inhibition of N-terminal His-tagged BRAF V600E mutant (unknown origin) expressed in baculovirus infected insect cells co-expressing CDC37 using biotinylated-MEK as substrate by AlphaScreen assay, IC50 = 0.013 μM.	29461827
A375	Function assay		Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by AlphaScreen assay, IC50 = 0.044 μM.	29461827
A375	Function assay		Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK, IC50 = 0.046 μM.	22808911
A375	Antiproliferative assay		Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50 = 0.5 μM.	22808911
HCT116	Antiproliferative assay		Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant, IC50 = 27 μM.	22808911
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
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生物活性

製品説明

Targets

C-Raf-1 (Y340D/Y341D) ^[1] (Cell-free assay)	B-Raf (V600E) ^[1] (Cell-free assay)	BRK ^[1] (Cell-free assay)	B-Raf ^[1] (Cell-free assay)
6.7 nM	13 nM	130 nM	160 nM

In Vitro
In vitro	PLX-4720 displays >10 times selectivity against wild type B-Raf, and >100 times selectivity over other kinases such as Frk, Src, Fak, FGFR, and Aurora A with IC50 of 1.3-3.4 μM. PLX-4720 significantly inhibits the ERK phosphorylation in cell lines bearing B-Raf^V600E with IC50 of 14-46 nM, but not the cells with wild-type B-Raf. PLX-4720 significantly inhibits the growth of tumor cell lines bearing the B-Raf^V600E oncogene, such as COLO205, A375, WM2664, and COLO829 with GI50 of 0.31 μM, 0.50 μM, 1.5 μM, and 1.7 μM, respectively. In addition, PLX-4720 treatment at 1 μM induces cell cycle arrest and apoptosis exclusively in the B-Raf^V600E-positive 1205Lu cells, but not in the B-Raf wild-type C8161 cells. ^[1] PLX-4720 treatment (10 μM) significantly induces >14-fold expression of BIM in the PTEN⁺ cells, compared with the PTEN- cell lines (4-fold), giving an explanation of the resistance of PTEN^- cells to PLX-4720-induced apoptosis. ^[2]
Kinase Assay	In vitro Raf kinase activities
Kinase Assay	The in vitro kinase activities of wild type Raf and mutants are determined by measuring phosphorylation of biotinylated-MEK protein using Perkin-Elmer's AlphaScreen Technology. For each enzyme (0.1 ng), 20-μL reactions are carried out in 20 mM Hepes (pH 7.0), 10 mM MgCl₂, 1 mM DTT, 0.01% Tween-20, 100 nM biotin-MEK protein, various ATP concentrations, and increasing concentrations of PLX-4720 at room temperature. Reactions are stopped at 2, 5, 8, 10, 20, and 30 minutes with 5 μL of a solution containing 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, and 0.3% BSA. The stop solution also includes phospho-MEK Antibody, Streptavidin-coated Donor beads and Protein A Acceptor beads from the AlphaScreen Protein A Detection Kit. The antibody and beads are preincubated in stop solution in the dark at room temperature for 30 minutes. The final dilution of antibody is 1/2,000, and the final concentration of each bead is 10 μg/mL. The assay plates are incubated at room temperature for one hour then are read on a PerkinElmer AlphaQuest reader.
細胞実験	細胞株	COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, and C8161 cells
	濃度	Dissolved in DMSO, final concentrations ~1 mM
	反応時間	24, 48, and 72 hours
	実験の流れ	Cells are treated with various concentrations PLX-4720 for 24, 48, and 72 hours. Cell proliferation is measured by using the CellTiter-Glo Luminescent Cell Viability Assay or MTT assay. For cell cycle analysis, supernatant and cells are collected, pelleted, and fixed with 70% ethanol. Before staining with propidium iodide (10 μg/mL), cells are incubated for 1 hour at 37 °C in 0.5 mg/mL RNase I to rid samples of residual RNA contamination. Samples are then analyzed by using the EPICS XL apparatus. For the assessment of apoptosis, media and cells are harvested and pelleted before staining with annexin-FITC and propidium iodide. Samples are subsequently analyzed by using the EPICS XL apparatus.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	pAkt(Ser473) / pAkt(Thr308) p27 / Cyclin D1 / pRb p-EGFR 1173 / EGFR / p-Akt / Akt p-MEK / MEK / p-ERK / ERK / p-FAK(S910)		21828154
	Immunofluorescence	ZKSCAN3 / TFEB LAMP1		30979895
	Growth inhibition assay	Cell viability		27848137
	ELISA	mIFN-γ		23204132

In Vivo
In Vivo	Oral administration of PLX-4720 at 20 mg/kg/day induces significant tumor growth delays and regressions in B-Raf^V600E-dependent COLO205 tumor xenografts, without obvious adverse effects in mice even at dose of 1 g/kg. PLX-4720 at 100 mg/kg twice daily almost completely eliminates the 1205Lu xenografts bearing B-Raf^V600E, while has no activity against C8161 xenografts bearing wild-type B-Raf. The anti-tumor effects of PLX-4720 correlate with the blockade of MAPK pathway in those cells harboring the V600E mutation. ^[1] PLX-4720 treatment at 30 mg/kg/day significant inhibits the tumor growth of 8505c xenografts by >90%, and dramatically decreases distant lung metastases. ^[3]
動物実験	動物モデル	Female athymic mice (NCr nu/nu) implanted s.c. with COLO205 cells, and SCID mice with 1205Lu or C8161 cells
	投与量	5, 20, or 100 mg/kg
	投与経路	Oral gavage once or twice daily

参考
[1] Tsai J, et al. Proc Natl Acad Sci U S A, 2008, 105(8), 3041-3046. [2] Paraiso KH, et al. Cancer Res, 2011, 71(7), 2750-2760. [3] Nucera C, et al. Proc Natl Acad Sci U S A, 2010, 107(23), 10649-10654.

参考

化学情報

分子量	413.83	化学式	C₁₇H₁₄ClF₂N₃O₃S
CAS No.	918505-84-7	SDF	Download PLX-4720 SDFをダウンロードする
Smiles	CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)Cl)F
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 83 mg/mL ( (200.56 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問（FAQ）

質問1:
What would you recommend to make working solution for intraperitoneal injection into mice?

回答
PLX4720 has very limited solubility in aqueous solution and for this reason, we recommend oral gavage to administer this compound as not fully dissolved suspension can be used in oral gavage feeding.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):