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PLX-4720 B-Raf 억제제

Name: PLX-4720
Brand: Selleck Chemicals
SKU: S1152
Rating: 5 (197 reviews)

제품 번호S1152

PLX4720은 B-Raf^V600E의 강력하고 선택적인 억제제로, 세포 없는 분석에서 IC50 13 nM이며, c-Raf-1(Y340D 및 Y341D 돌연변이)과 동등하게 강력하고, 야생형 B-Raf보다 B-RafV600E에 대해 10배 선택성을 갖습니다.

화학 구조

분자량: 413.83

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품질 관리

배치: 순도: 99.98%

99.98

함께 자주 사용되는 제품 PLX-4720

Dactolisib (BEZ235)

Treatment with this compound and Dactolisib decreases both pERK and pAKT levels in Colo-205 xenografts.

Navitoclax (ABT-263)

It and Navitoclax can enhance the clinical efficacy of BRAF inhibitors.

NMS-E973

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

SB431542

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

관련 타겟	ERK p38 MAPK JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
기타 Raf 억제제	LY3009120 Exarafenib (KIN-2787) GDC-0879 Avutometinib (Ro5126766, CH5126766) AZ 628 SB590885 TAK-632 GW5074 RAF265 (CHIR-265) PLX8394 (Plixorafenib, FORE8394)

세포 배양, 처리 및 작업 농도

세포주	분석 유형	배양 시간	활성 설명	PMID
DU-4475	Growth Inhibition Assay		IC50=0.07457 μM	SANGER
EoL-1-cell	Growth Inhibition Assay		IC50=0.14166 μM	SANGER
C32	Growth Inhibition Assay		IC50=0.15131 μM	SANGER
M14	Growth Inhibition Assay		IC50=0.21757 μM	SANGER
CP50-MEL-B	Growth Inhibition Assay		IC50=0.29784 μM	SANGER
A101D	Growth Inhibition Assay		IC50=0.32589 μM	SANGER
G-361	Growth Inhibition Assay		IC50=0.34637 μM	SANGER
HT-144	Growth Inhibition Assay		IC50=0.36329 μM	SANGER
ACN	Growth Inhibition Assay		IC50=0.38477 μM	SANGER
COLO-829	Growth Inhibition Assay		IC50=0.38968 μM	SANGER
MEL-HO	Growth Inhibition Assay		IC50=0.41179 μM	SANGER
SH-4	Growth Inhibition Assay		IC50=0.41422 μM	SANGER
SK-MEL-3	Growth Inhibition Assay		IC50=0.51568 μM	SANGER
A375	Growth Inhibition Assay		IC50=0.67359 μM	SANGER
MMAC-SF	Growth Inhibition Assay		IC50=0.68614 μM	SANGER
BHT-101	Growth Inhibition Assay		IC50=0.70702 μM	SANGER
K5	Growth Inhibition Assay		IC50=0.76148 μM	SANGER
BV-173	Growth Inhibition Assay		IC50=0.79644 μM	SANGER
RVH-421	Growth Inhibition Assay		IC50=0.86796 μM	SANGER
HCC2218	Growth Inhibition Assay		IC50=0.87844 μM	SANGER
WM-115	Growth Inhibition Assay		IC50=0.88692 μM	SANGER
SK-MEL-28	Growth Inhibition Assay		IC50=1.04569 μM	SANGER
COLO-679	Growth Inhibition Assay		IC50=1.10464 μM	SANGER
MZ7-mel	Growth Inhibition Assay		IC50=1.14963 μM	SANGER
SK-MEL-30	Growth Inhibition Assay		IC50=1.33386 μM	SANGER
NCI-H209	Growth Inhibition Assay		IC50=1.6086 μM	SANGER
HTC-C3	Growth Inhibition Assay		IC50=1.66294 μM	SANGER
KARPAS-45	Growth Inhibition Assay		IC50=2.04978 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay		IC50=2.11969 μM	SANGER
KP-4	Growth Inhibition Assay		IC50=2.30787 μM	SANGER
PA-1	Growth Inhibition Assay		IC50=2.72673 μM	SANGER
HuO-3N1	Growth Inhibition Assay		IC50=2.87946 μM	SANGER
NCI-H358	Growth Inhibition Assay		IC50=2.92232 μM	SANGER
CTB-1	Growth Inhibition Assay		IC50=3.40176 μM	SANGER
697	Growth Inhibition Assay		IC50=3.55266 μM	SANGER
CP66-MEL	Growth Inhibition Assay		IC50=4.15927 μM	SANGER
NB13	Growth Inhibition Assay		IC50=4.49179 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay		IC50=4.53325 μM	SANGER
A2058	Growth Inhibition Assay		IC50=4.72164 μM	SANGER
KG-1	Growth Inhibition Assay		IC50=4.73908 μM	SANGER
8305C	Growth Inhibition Assay		IC50=5.1873 μM	SANGER
RPMI-7951	Growth Inhibition Assay		IC50=5.80283 μM	SANGER
CHL-1	Growth Inhibition Assay		IC50=5.97603 μM	SANGER
TI-73	Growth Inhibition Assay		IC50=6.00902 μM	SANGER
HT-1080	Growth Inhibition Assay		IC50=6.10946 μM	SANGER
ES5	Growth Inhibition Assay		IC50=6.14924 μM	SANGER
8-MG-BA	Growth Inhibition Assay		IC50=6.18129 μM	SANGER
NB7	Growth Inhibition Assay		IC50=6.21373 μM	SANGER
H4	Growth Inhibition Assay		IC50=6.22493 μM	SANGER
CAL-72	Growth Inhibition Assay		IC50=6.45423 μM	SANGER
HCC1806	Growth Inhibition Assay		IC50=6.81931 μM	SANGER
BCPAP	Growth Inhibition Assay		IC50=7.21764 μM	SANGER
LB2241-RCC	Growth Inhibition Assay		IC50=7.36907 μM	SANGER
COLO-741	Growth Inhibition Assay		IC50=8.01679 μM	SANGER
HSC-3	Growth Inhibition Assay		IC50=8.07068 μM	SANGER
SW982	Growth Inhibition Assay		IC50=8.41516 μM	SANGER
GCT	Growth Inhibition Assay		IC50=8.75314 μM	SANGER
KY821	Growth Inhibition Assay		IC50=9.05178 μM	SANGER
JVM-3	Growth Inhibition Assay		IC50=9.56999 μM	SANGER
RS4-11	Growth Inhibition Assay		IC50=9.6048 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay		IC50=10.0149 μM	SANGER
A431	Growth Inhibition Assay		IC50=10.4212 μM	SANGER
LXF-289	Growth Inhibition Assay		IC50=10.458 μM	SANGER
SK-MEL-24	Growth Inhibition Assay		IC50=10.8274 μM	SANGER
NOS-1	Growth Inhibition Assay		IC50=10.8472 μM	SANGER
KNS-62	Growth Inhibition Assay		IC50=11.2404 μM	SANGER
SK-HEP-1	Growth Inhibition Assay		IC50=11.3527 μM	SANGER
A3-KAW	Growth Inhibition Assay		IC50=11.7178 μM	SANGER
SK-LU-1	Growth Inhibition Assay		IC50=12.2655 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
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
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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	413.83	화학식	C₁₇H₁₄ClF₂N₃O₃S	보관 (수령일로부터)	3년-20°C분말
CAS 번호	918505-84-7	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)Cl)F

용해도

In vitro
배치:

DMSO : 83 mg/mL (200.56 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 82 mg/mL (198.14 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 82 mg/mL (198.14 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 83 mg/mL (200.56 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 83 mg/mL (200.56 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC₅₀/Ki	C-Raf-1 (Y340D/Y341D) (Cell-free assay) 6.7 nM B-Raf (V600E) (Cell-free assay) 13 nM BRK (Cell-free assay) 130 nM B-Raf (Cell-free assay) 160 nM
시험관 내(In vitro)	PLX-4720은 야생형 B-Raf에 대해 10배 이상의 선택성을 보이며, Frk, Src, Fak, FGFR, Aurora A와 같은 다른 키나아제에 대해서는 100배 이상의 선택성을 보이며 IC50은 1.3-3.4 μM입니다. 이 화합물은 B-Raf^V600E를 발현하는 세포주에서 ERK 인산화를 IC50 14-46 nM로 유의하게 억제하지만, 야생형 B-Raf를 가진 세포에서는 그렇지 않습니다. COLO205, A375, WM2664, COLO829와 같은 B-Raf^V600E 종양유전자를 발현하는 종양 세포주의 성장을 각각 GI50 0.31 μM, 0.50 μM, 1.5 μM, 1.7 μM으로 유의하게 억제합니다. 또한, 1 μM의 이 화학적 처리는 B-Raf^V600E 양성 1205Lu 세포에서만 세포 주기 정지 및 세포 사멸을 유도하며, B-Raf 야생형 C8161 세포에서는 유도하지 않습니다. 이 화합물 처리(10 μM)는 PTEN- 세포주(4배)와 비교하여 PTEN⁺ 세포에서 BIM 발현을 14배 이상 유의하게 유도하여, PTEN^- 세포가 이 화학적 유도 세포 사멸에 저항하는 이유를 설명합니다.
키나아제 분석	시험관 내 Raf 키나아제 활성
키나아제 분석	야생형 Raf 및 돌연변이의 시험관 내 키나아제 활성은 Perkin-Elmer의 AlphaScreen 기술을 사용하여 바이오틴화된 MEK 단백질의 인산화를 측정하여 결정됩니다. 각 효소(0.1 ng)에 대해 20 mM Hepes (pH 7.0), 10 mM MgCl₂, 1 mM DTT, 0.01% Tween-20, 100 nM 바이오틴-MEK 단백질, 다양한 ATP 농도 및 증가하는 PLX-4720 농도에서 실온에서 20 μL 반응이 수행됩니다. 반응은 2, 5, 8, 10, 20 및 30분 후에 20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA 및 0.3% BSA를 포함하는 5 μL 용액으로 중단됩니다. 중단 용액에는 또한 phospho-MEK 항체, 스트렙타비딘 코팅된 도너 비드 및 AlphaScreen Protein A Detection Kit의 프로테인 A 억셉터 비드가 포함됩니다. 항체와 비드는 실온에서 어둠 속에서 30분 동안 중단 용액에서 사전 배양됩니다. 항체의 최종 희석은 1/2,000이며, 각 비드의 최종 농도는 10 μg/mL입니다. 분석 플레이트는 실온에서 1시간 동안 배양된 후 PerkinElmer AlphaQuest 리더에서 판독됩니다.
생체 내(In vivo)	PLX-4720을 20 mg/kg/day 경구 투여하면 B-Raf^V600E 의존성 COLO205 종양 이종이식편에서 유의미한 종양 성장 지연 및 퇴행을 유도하며, 1 g/kg 용량에서도 쥐에게 명백한 부작용은 없습니다. 이 화합물을 100 mg/kg씩 하루 두 번 투여하면 B-Raf^V600E를 발현하는 1205Lu 이종이식편을 거의 완전히 제거하는 반면, 야생형 B-Raf를 발현하는 C8161 이종이식편에 대해서는 활성이 없습니다. 이 화합물의 항종양 효과는 V600E 돌연변이를 가진 세포에서 MAPK 경로의 차단과 관련이 있습니다. 30 mg/kg/day의 이 화학적 처리는 8505c 이종이식편의 종양 성장을 90% 이상 유의하게 억제하고 원격 폐 전이를 극적으로 감소시킵니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/18287029/ [2] https://pubmed.ncbi.nlm.nih.gov/21317224/ [3] https://pubmed.ncbi.nlm.nih.gov/20498063/

적용 분야

방법	바이오마커	PMID
Western blot	p-MEK / MEK / p-ERK / ERK / p-FAK(S910) p-EGFR 1173 / EGFR / p-Akt / Akt p27 / Cyclin D1 / pRb pAkt(Ser473) / pAkt(Thr308)	23076151
Immunofluorescence	LAMP1 ZKSCAN3 / TFEB	30979895
Growth inhibition assay	Cell viability	27848137
ELISA	mIFN-γ	23204132

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