연구용

PF-4708671 S6 Kinase 억제제

Name: PF-4708671
Brand: Selleck Chemicals
SKU: S2163
Rating: 5 (59 reviews)

제품 번호S2163

PF-4708671은 세포 투과성 p70 ribosomal S6 kinase (S6K1 isoform) 억제제로, 무세포 분석에서 K_i/IC50가 20 nM/160 nM이며, S6K2보다 S6K1에 대해 400배, MSK1 및 RSK1/2보다 S6K1에 대해 각각 4배 및 >20배 더 높은 선택성을 보입니다. 이 화합물은 Autophagy를 유도합니다. 보고된 최초의 S6K1 특이적 억제제입니다.

PF-4708671 S6 Kinase 억제제 Chemical Structure

화학 구조

분자량: 390.41

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품질 관리

배치: 순도: 99.97%

99.97

관련 타겟	PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A
기타 S6 Kinase 억제제	BI-D1870 LY2584702 LY2584702 Tosylate LJH685 LJI308 S6K-18 3'-Hydroxypterostilbene L-Norvaline BRD7389 Gingerenone A

세포 배양, 처리 및 작업 농도

세포주	분석 유형	활성 설명
BHT-101	Growth Inhibition Assay	IC50=0.82024 μM
UACC-893	Growth Inhibition Assay	IC50=5.19886 μM
A427	Growth Inhibition Assay	IC50=5.72567 μM
OCUB-M	Growth Inhibition Assay	IC50=6.66102 μM
SW684	Growth Inhibition Assay	IC50=7.52268 μM
SK-LMS-1	Growth Inhibition Assay	IC50=9.01302 μM
CP50-MEL-B	Growth Inhibition Assay	IC50=9.30419 μM
NCI-H1651	Growth Inhibition Assay	IC50=10.0276 μM
ABC-1	Growth Inhibition Assay	IC50=10.1037 μM
OE19	Growth Inhibition Assay	IC50=10.1733 μM
DSH1	Growth Inhibition Assay	IC50=10.8879 μM
SW13	Growth Inhibition Assay	IC50=11.9319 μM
MDA-MB-453	Growth Inhibition Assay	IC50=12.1603 μM
647-V	Growth Inhibition Assay	IC50=12.3582 μM
NCI-H2342	Growth Inhibition Assay	IC50=12.3995 μM
LB2241-RCC	Growth Inhibition Assay	IC50=12.5779 μM
UACC-257	Growth Inhibition Assay	IC50=13.4453 μM
NCI-H661	Growth Inhibition Assay	IC50=13.6449 μM
FADU	Growth Inhibition Assay	IC50=13.6992 μM
A2780	Growth Inhibition Assay	IC50=13.8041 μM
NCI-H1793	Growth Inhibition Assay	IC50=14.4085 μM
TE-8	Growth Inhibition Assay	IC50=15.3465 μM
HGC-27	Growth Inhibition Assay	IC50=16.1644 μM
MMAC-SF	Growth Inhibition Assay	IC50=17.3727 μM
Calu-6	Growth Inhibition Assay	IC50=18.1513 μM
HUTU-80	Growth Inhibition Assay	IC50=18.3959 μM
SAS	Growth Inhibition Assay	IC50=18.6455 μM
IST-MES1	Growth Inhibition Assay	IC50=18.6508 μM
C3A	Growth Inhibition Assay	IC50=18.7919 μM
ES3	Growth Inhibition Assay	IC50=18.8364 μM
HSC-2	Growth Inhibition Assay	IC50=19.6541 μM
T47D	Growth Inhibition Assay	IC50=20.1485 μM
EW-7	Growth Inhibition Assay	IC50=20.8588 μM
LN-405	Growth Inhibition Assay	IC50=20.8965 μM
U031	Growth Inhibition Assay	IC50=21.4802 μM
A549	Growth Inhibition Assay	IC50=21.8491 μM
RMG-I	Growth Inhibition Assay	IC50=22.2668 μM
BT-474	Growth Inhibition Assay	IC50=22.6551 μM
NB69	Growth Inhibition Assay	IC50=23.152 μM
NB7	Growth Inhibition Assay	IC50=24.188 μM
HCC1569	Growth Inhibition Assay	IC50=24.6125 μM
MEL-JUSO	Growth Inhibition Assay	IC50=24.6908 μM
MDA-MB-175-VII	Growth Inhibition Assay	IC50=25.2517 μM
HCC1419	Growth Inhibition Assay	IC50=25.6003 μM
Ca9-22	Growth Inhibition Assay	IC50=25.6432 μM
KGN	Growth Inhibition Assay	IC50=25.7547 μM
LB373-MEL-D	Growth Inhibition Assay	IC50=26.1938 μM
NCI-H1755	Growth Inhibition Assay	IC50=26.8841 μM
D-423MG	Growth Inhibition Assay	IC50=27.0715 μM
DK-MG	Growth Inhibition Assay	IC50=28.7846 μM
NCI-H1623	Growth Inhibition Assay	IC50=28.8342 μM
KU-19-19	Growth Inhibition Assay	IC50=28.995 μM
C-33-A	Growth Inhibition Assay	IC50=29.2198 μM
SCC-4	Growth Inhibition Assay	IC50=30.3354 μM
MG-63	Growth Inhibition Assay	IC50=30.5994 μM
LNCaP-Clone-FGC	Growth Inhibition Assay	IC50=31.4921 μM
CAPAN-1	Growth Inhibition Assay	IC50=31.5286 μM
GI-ME-N	Growth Inhibition Assay	IC50=31.5353 μM
RERF-LC-MS	Growth Inhibition Assay	IC50=32.6747 μM
KLE	Growth Inhibition Assay	IC50=33.4334 μM
KNS-81-FD	Growth Inhibition Assay	IC50=33.5008 μM
DOK	Growth Inhibition Assay	IC50=34.6612 μM
ACHN	Growth Inhibition Assay	IC50=35.1588 μM
KYSE-520	Growth Inhibition Assay	IC50=35.2361 μM
SBC-5	Growth Inhibition Assay	IC50=35.5116 μM
NCI-H28	Growth Inhibition Assay	IC50=35.6695 μM
ES7	Growth Inhibition Assay	IC50=36.2249 μM
A172	Growth Inhibition Assay	IC50=36.4187 μM
UM-UC-3	Growth Inhibition Assay	IC50=37.8746 μM
LXF-289	Growth Inhibition Assay	IC50=38.0047 μM
KP-4	Growth Inhibition Assay	IC50=38.4739 μM
TE-1	Growth Inhibition Assay	IC50=39.6589 μM
G-402	Growth Inhibition Assay	IC50=40.061 μM
786-0	Growth Inhibition Assay	IC50=40.9096 μM
K5	Growth Inhibition Assay	IC50=41.3686 μM
SK-N-DZ	Growth Inhibition Assay	IC50=41.3823 μM
OVCAR-4	Growth Inhibition Assay	IC50=41.7568 μM
T84	Growth Inhibition Assay	IC50=42.1263 μM
GCIY	Growth Inhibition Assay	IC50=43.0803 μM
BB49-HNC	Growth Inhibition Assay	IC50=43.3348 μM
SNU-C2B	Growth Inhibition Assay	IC50=43.6436 μM
TE-6	Growth Inhibition Assay	IC50=43.8894 μM
23132-87	Growth Inhibition Assay	IC50=44.2978 μM
DMS-53	Growth Inhibition Assay	IC50=44.3384 μM
ONS-76	Growth Inhibition Assay	IC50=44.7661 μM
DMS-273	Growth Inhibition Assay	IC50=44.943 μM
COLO-824	Growth Inhibition Assay	IC50=45.8775 μM
DMS-114	Growth Inhibition Assay	IC50=45.8927 μM
YKG-1	Growth Inhibition Assay	IC50=46.0355 μM
RH-18	Growth Inhibition Assay	IC50=46.3733 μM
NCI-H1355	Growth Inhibition Assay	IC50=46.618 μM
NCI-H2170	Growth Inhibition Assay	IC50=47.7584 μM
OC-314	Growth Inhibition Assay	IC50=47.8478 μM
NCI-H2030	Growth Inhibition Assay	IC50=47.8906 μM
22RV1	Growth Inhibition Assay	IC50=47.9015 μM
G-401	Growth Inhibition Assay	IC50=48.4415 μM
YAPC	Growth Inhibition Assay	IC50=49.8073 μM
SW1573	Growth Inhibition Assay	IC50=50.2435 μM
COLO-792	Growth Inhibition Assay	IC50=50.6237 μM
KNS-62	Growth Inhibition Assay	IC50=50.7508 μM
NB5	Growth Inhibition Assay	IC50=51.4509 μM
CP66-MEL	Growth Inhibition Assay	IC50=51.6408 μM
CaR-1	Growth Inhibition Assay	IC50=52.0606 μM
CAL-54	Growth Inhibition Assay	IC50=52.1102 μM
8305C	Growth Inhibition Assay	IC50=52.315 μM
Calu-3	Growth Inhibition Assay	IC50=52.3733 μM
AU565	Growth Inhibition Assay	IC50=52.5509 μM
CW-2	Growth Inhibition Assay	IC50=52.8654 μM
BEN	Growth Inhibition Assay	IC50=53.7862 μM
NCI-H1975	Growth Inhibition Assay	IC50=53.8966 μM
HCT-116	Growth Inhibition Assay	IC50=54.0327 μM
SH-4	Growth Inhibition Assay	IC50=54.138 μM
NCI-H1693	Growth Inhibition Assay	IC50=54.2103 μM
BPH-1	Growth Inhibition Assay	IC50=55.2892 μM
CAMA-1	Growth Inhibition Assay	IC50=55.8116 μM
A388	Growth Inhibition Assay	IC50=56.0985 μM
C2BBe1	Growth Inhibition Assay	IC50=56.2634 μM
GAMG	Growth Inhibition Assay	IC50=56.5955 μM
MKN28	Growth Inhibition Assay	IC50=56.8013 μM
VA-ES-BJ	Growth Inhibition Assay	IC50=56.8745 μM
HuCCT1	Growth Inhibition Assay	IC50=57.0492 μM
BFTC-905	Growth Inhibition Assay	IC50=57.2898 μM
LS-123	Growth Inhibition Assay	IC50=57.5668 μM
LB996-RCC	Growth Inhibition Assay	IC50=58.0287 μM
NCI-H1048	Growth Inhibition Assay	IC50=58.2188 μM
COR-L105	Growth Inhibition Assay	IC50=58.7337 μM
OVCAR-8	Growth Inhibition Assay	IC50=59.1716 μM
SK-N-FI	Growth Inhibition Assay	IC50=59.3207 μM
MES-SA	Growth Inhibition Assay	IC50=59.4509 μM
SCC-9	Growth Inhibition Assay	IC50=59.4753 μM
EFO-27	Growth Inhibition Assay	IC50=59.943 μM
GT3TKB	Growth Inhibition Assay	IC50=60.6048 μM
HCC38	Growth Inhibition Assay	IC50=61.4379 μM
MLMA	Growth Inhibition Assay	IC50=61.6163 μM
D-566MG	Growth Inhibition Assay	IC50=63.5224 μM
SF295	Growth Inhibition Assay	IC50=63.6655 μM
ES4	Growth Inhibition Assay	IC50=64.4719 μM
CAKI-1	Growth Inhibition Assay	IC50=64.5721 μM
OAW-28	Growth Inhibition Assay	IC50=64.9647 μM
NCI-H460	Growth Inhibition Assay	IC50=65.0897 μM
JAR	Growth Inhibition Assay	IC50=65.5516 μM
SNU-449	Growth Inhibition Assay	IC50=65.7616 μM
D-392MG	Growth Inhibition Assay	IC50=65.9434 μM
EW-22	Growth Inhibition Assay	IC50=66.395 μM
GCT	Growth Inhibition Assay	IC50=67.0443 μM
NOS-1	Growth Inhibition Assay	IC50=67.6867 μM
RH-1	Growth Inhibition Assay	IC50=68.5559 μM
HuH-7	Growth Inhibition Assay	IC50=69.1002 μM
NUGC-3	Growth Inhibition Assay	IC50=70.9644 μM
IST-SL1	Growth Inhibition Assay	IC50=71.2324 μM
SHP-77	Growth Inhibition Assay	IC50=72.119 μM
SW1116	Growth Inhibition Assay	IC50=72.1407 μM
LK-2	Growth Inhibition Assay	IC50=72.8612 μM
U-2-OS	Growth Inhibition Assay	IC50=73.1828 μM
KYSE-150	Growth Inhibition Assay	IC50=73.6118 μM
U251	Growth Inhibition Assay	IC50=73.8168 μM
HT-1080	Growth Inhibition Assay	IC50=74.2574 μM
NCI-H1437	Growth Inhibition Assay	IC50=74.6326 μM
HPAF-II	Growth Inhibition Assay	IC50=74.6415 μM
Becker	Growth Inhibition Assay	IC50=75.1105 μM
PANC-10-05	Growth Inhibition Assay	IC50=75.2865 μM
TYK-nu	Growth Inhibition Assay	IC50=75.3102 μM
SKG-IIIa	Growth Inhibition Assay	IC50=75.3341 μM
NCI-H1993	Growth Inhibition Assay	IC50=75.7397 μM
S-117	Growth Inhibition Assay	IC50=75.755 μM
HuO9	Growth Inhibition Assay	IC50=76.0048 μM
CAL-51	Growth Inhibition Assay	IC50=76.1006 μM
BT-20	Growth Inhibition Assay	IC50=76.2168 μM
LB831-BLC	Growth Inhibition Assay	IC50=76.3217 μM
LB1047-RCC	Growth Inhibition Assay	IC50=76.7619 μM
ES8	Growth Inhibition Assay	IC50=78.0073 μM
UMC-11	Growth Inhibition Assay	IC50=78.0884 μM
NCI-H226	Growth Inhibition Assay	IC50=78.1315 μM
IGROV-1	Growth Inhibition Assay	IC50=78.555 μM
BHY	Growth Inhibition Assay	IC50=79.596 μM
MKN45	Growth Inhibition Assay	IC50=80.3174 μM
IA-LM	Growth Inhibition Assay	IC50=80.3511 μM
WM-115	Growth Inhibition Assay	IC50=81.4114 μM
VMRC-RCZ	Growth Inhibition Assay	IC50=81.4425 μM
NCI-H2291	Growth Inhibition Assay	IC50=81.6842 μM
MCF7	Growth Inhibition Assay	IC50=83.2897 μM
639-V	Growth Inhibition Assay	IC50=84.6129 μM
RT4	Growth Inhibition Assay	IC50=85.2403 μM
NCI-H2405	Growth Inhibition Assay	IC50=85.2997 μM
CAL-33	Growth Inhibition Assay	IC50=85.6315 μM
BT-549	Growth Inhibition Assay	IC50=85.9382 μM
HT-1197	Growth Inhibition Assay	IC50=88.1077 μM
G-361	Growth Inhibition Assay	IC50=88.1474 μM
LS-411N	Growth Inhibition Assay	IC50=89.3388 μM
HT-144	Growth Inhibition Assay	IC50=89.5992 μM
DJM-1	Growth Inhibition Assay	IC50=89.8845 μM
CAL-12T	Growth Inhibition Assay	IC50=90.7895 μM
MKN7	Growth Inhibition Assay	IC50=91.3551 μM
HuP-T3	Growth Inhibition Assay	IC50=96.1004 μM
SK-MG-1	Growth Inhibition Assay	IC50=96.1348 μM
NCI-H2347	Growth Inhibition Assay	IC50=98.1042 μM
SW872	Growth Inhibition Assay	IC50=100.456 μM
COLO-829	Growth Inhibition Assay	IC50=100.553 μM
MC-IXC	Growth Inhibition Assay	IC50=100.615 μM
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	390.41	화학식	C₁₉H₂₁F₃N₆	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1255517-76-0	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F

용해도

In vitro
배치:

DMSO : 30 mg/mL (76.84 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 8 mg/mL

Water : Insoluble

Ethanol : 40 mg/mL

DMSO : 30 mg/mL (76.84 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

DMSO : 30 mg/mL (76.84 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 8 mg/mL

Water : Insoluble

DMSO : 38 mg/mL (97.33 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 10 mg/mL

Water : 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.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	30.000mg/ml (76.84mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	5.000mg/ml (12.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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	p70 S6K1 (Cell-free assay) 160 nM
시험관 내(In vitro)	PF-4708671은 피페라지닐-피리미딘 유사체이며 최초의 S6K1 특이적 억제제입니다. 이 화합물은 밀접하게 관련된 S6K2 isoform 또는 다른 여러 AGC 키나제(Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 또는 SGK1)의 활성을 유의미하게 억제하지 않습니다. IGF-1(insulin-like growth factor 1) 반응에서 S6K1 매개 S6 단백질의 인산화를 방지하며, 매우 유사한 RSK(p90 ribosomal S6 kinase) 및 MSK(mitogen- and stress-activated kinase) 키나제의 PMA 유도 기질 인산화에는 영향을 미치지 않습니다. 이 화학 물질은 또한 S6K1의 T-루프 및 소수성 모티프의 인산화를 유도하는 것으로 밝혀졌으며, 이 효과는 mTORC1(mTOR complex 1)에 의존합니다. mTORC1의 활성에는 영향을 미치지 않습니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/20704563/

적용 분야

방법	바이오마커	이미지	PMID
Western blot	p-mTOR / mTOR / p-p70S6K / p70S6K pS6 / S6 / pS6K / S6K1 / pAKT / AKT		30423811
Growth inhibition assay	Cell viability		30423811

기술 지원

취급 설명서

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자주 묻는 질문

질문 1:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for it is suitable for i.p. or not?

답변:
The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one for this compound. It is a suspension.

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):