|N-(3-(5-氯-1H-吡咯并[2,3-b]吡啶-3-羰基)-2,4-二氟苯基)丙烷-1-磺酰胺|CsnPharm

CAS No.: 918505-84-7

N-(3-(5-Chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide Catalog No. CSN12391

Synonyms: Raf Kinase Inhibitor V

PLX 4720 is a potent and selective inhibitor of B-RafV600E (IC50=13 nM) and c-Raf-1Y340D/Y341D (IC50=6.7 nM), whth a 10-fold selectivity for B-RafV600E than wild-type B-Raf.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. PLX4720 is a potent and selective inhibitor of B-Raf_V600E mutant, with less potent to wt-braf and BRK with IC50 values of 160nM and 130nM, and showed selectivity to B-Raf_V600E mutant over 100 fold against a diverse panel of 70 other kinases. Consistent with the in vitro study, PLX4720 showed more potent anti-proliferation in tumor cell lines bearing the B-Raf_V600E oncogene with GI50<1.7μM,such as COLO205, A375, WM2664 and COLO829 cells, versus GI50>10μM on cells with wt-braf. PLX4720 initiates antimelanoma activity, inhibition of MAPK pathway represented suppressed p-ERK, apoptotic response only in cells harboring the V600E mutation. Daily oral gavage of PLX4720, at dose of 20mg/kg 14 days resulted in substantial block of tumor growth and a 21-day tumor growth delay, with ERK phosphorylation inhibited by 43% in treated tumors, in COLO205 xenograft model^[1].
作用机制PLX4720 is an ATP competitive kinase inhibitor.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
23132-87	-	Growth Inhibition Assay	-	IC50=19.7642 μM	SANGER
5637	-	Growth Inhibition Assay	-	IC50=20.0478 μM	SANGER
697	-	Growth Inhibition Assay	-	IC50=3.55266 μM	SANGER

更多
动物研究
剂量
Mice: 5 mg/kg - 20 mg/kg, max = 1000 mg/kg^[1] (p.o.)

给药途径
p.o.

动物研究
剂量	Mice: 5 mg/kg - 20 mg/kg, max = 1000 mg/kg^[1] (p.o.)
给药途径	p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4165 mL
- 12.0824 mL
- 24.1647 mL
- 5 mM
- 0.4833 mL
- 2.4165 mL
- 4.8329 mL
- 10 mM
- 0.2416 mL
- 1.2082 mL
- 2.4165 mL

技术信息

CAS号

918505-84-7

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H14ClF2N3O3S

运输

蓝冰

分子量

413.83

别名

Raf Kinase Inhibitor V

溶解度

DMSO	83.0 mg/mL (200.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

2% DMSO+50% PEG 300+5% Tween 80+water

5 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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

N-(3-(5-Chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide Catalog No. CSN12391

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