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Serdemetan (JNJ-26854165) p53 활성제

Name: Serdemetan (JNJ-26854165)
Brand: Selleck Chemicals
SKU: S1172
Rating: 5 (15 reviews)

제품 번호S1172

Serdemetan (JNJ-26854165)은 HDM2 유비퀴틴 E3 Ligase 길항제로 작용하며 p53 야생형 세포에서 초기 Apoptosis를 유도하고, 기능성 p53이 없는 경우 지연된 Apoptosis에 이어 세포 증식을 억제합니다. 1상.

Serdemetan (JNJ-26854165) p53 활성제 Chemical Structure

화학 구조

분자량: 328.41

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품질 관리

배치: 순도: 99.62%

99.62

관련 타겟	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
기타 p53 억제제	Eprenetapopt (APR-246) CBL0137 Hydrochloride Pifithrin-α (PFTα) Hhydrobromide Pifithrin-μ RITA PRIMA-1 NSC 319726 (ZMC1) NSC348884 Tenovin-6 Tenovin-1

세포 배양, 처리 및 작업 농도

세포주	분석 유형	활성 설명
KU-19-19 cell	Growth inhibition assay	Inhibition of human KU-19-19 cell growth in a cell viability assay, IC50=0.93236 μM
H4 cell	Growth inhibition assay	Inhibition of human H4 cell growth in a cell viability assay, IC50=1.06707 μM
KGN cell	Growth inhibition assay	Inhibition of human KGN cell growth in a cell viability assay, IC50=1.6205 μM
786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.72989 μM
769-P cell	Growth inhibition assay	Inhibition of human 769-P cell growth in a cell viability assay, IC50=1.82224 μM
K5 cell	Growth inhibition assay	Inhibition of human K5 cell growth in a cell viability assay, IC50=2.01624 μM
MLMA cell	Growth inhibition assay	Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=2.03217 μM
MLMA cell	Growth inhibition assay	Inhibition of human MLMA cell growth in a cell viability assay, IC50=2.28703 μM
EW-7 cell	Growth inhibition assay	Inhibition of human EW-7 cell growth in a cell viability assay, IC50=2.32695 μM
SW1088 cell	Growth inhibition assay	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.80651 μM
MC-IXC cell	Growth inhibition assay	Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=2.87792 μM
NCI-H2052 cell	Growth inhibition assay	Inhibition of human NCI-H2052 cell growth in a cell viability assay, IC50=3.08157 μM
IGR-1 cell	Growth inhibition assay	Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=3.12028 μM
DSH1 cell	Growth inhibition assay	Inhibition of human DSH1 cell growth in a cell viability assay, IC50=3.24296 μM
PA-1 cell	Growth inhibition assay	Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.30059μM
SK-MEL-3 cell	Growth inhibition assay	Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=3.31207 μM
SW900 cell	Growth inhibition assay	Inhibition of human SW900 cell growth in a cell viability assay, IC50=3.48255 μM
CAKI-1 cell	Growth inhibition assay	Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=3.52738 μM
ES1 cell	Growth inhibition assay	Inhibition of human ES1 cell growth in a cell viability assay, IC50=3.52897 μM
SK-N-DZ cell	Growth inhibition assay	Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=3.62595 μM
RH-1 cell	Growth inhibition assay	Inhibition of human RH-1 cell growth in a cell viability assay, IC50=3.68463 μM
ES8 cell	Growth inhibition assay	Inhibition of human ES8 cell growth in a cell viability assay, IC50=3.69702 μM
NEC8 cell	Growth inhibition assay	Inhibition of human NEC8 cell growth in a cell viability assay, IC50=3.76982 μM
LNCaP-Clone-FGC cell	Growth inhibition assay	Inhibition of human LNCaP-Clone-FGC cell growth in a cell viability assay, IC50=3.83536 μM
HCE-4 cell	Growth inhibition assay	Inhibition of human HCE-4 cell growth in a cell viability assay, IC50=3.9807 μM
U-118-MG cell	Growth inhibition assay	Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=4.01066 μM
GI-ME-N cell	Growth inhibition assay	Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=4.08796 μM
LB1047-RCC cell	Growth inhibition assay	Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=4.16143 μM
HT-1080 cell	Growth inhibition assay	Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=4.19921 μM
NB69 cell	Growth inhibition assay	Inhibition of human NB69 cell growth in a cell viability assay, IC50=4.35047 μM
NCI-H1693 cell	Growth inhibition assay	Inhibition of human NCI-H1693 cell growth in a cell viability assay, IC50=4.44895 μM
HSC-3 cell	Growth inhibition assay	Inhibition of human HSC-3 cell growth in a cell viability assay, IC50=4.49933 μM
MDA-MB-231 cell	Growth inhibition assay	Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50=4.55899 μM
HOS cell	Growth inhibition assay	Inhibition of human HOS cell growth in a cell viability assay, IC50=4.7863 μM
BT-549 cell	Growth inhibition assay	Inhibition of human BT-549 cell growth in a cell viability assay, IC50=4.7887 μM
NB17 cell	Growth inhibition assay	Inhibition of human NB17 cell growth in a cell viability assay, IC50=4.78976 μM
5637 cell	Growth inhibition assay	Inhibition of human 5637 cell growth in a cell viability assay, IC50=4.79652 μM
OVCAR-8 cell	Growth inhibition assay	Inhibition of human OVCAR-8 cell growth in a cell viability assay, IC50=4.92436 μM
G-402 cell	Growth inhibition assay	Inhibition of human G-402 cell growth in a cell viability assay, IC50=4.93035 μM
BB30-HNC cell	Growth inhibition assay	Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=5.07218 μM
HCC1806 cell	Growth inhibition assay	Inhibition of human HCC1806 cell growth in a cell viability assay, IC50=5.08339 μM
COLO-800 cell	Growth inhibition assay	Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=5.1264 μM
FADU cell	Growth inhibition assay	Inhibition of human FADU cell growth in a cell viability assay, IC50=5.36557 μM
NCI-H1651 cell	Growth inhibition assay	Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=5.39409 μM
AGS cell	Growth inhibition assay	Inhibition of human AGS cell growth in a cell viability assay, IC50=5.47711 μM
CHP-212 cell	Growth inhibition assay	Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=5.39409 μM
YAPC cell	Growth inhibition assay	Inhibition of human YAPC cell growth in a cell viability assay, IC50=5.47711 μM
GOTO cell	Growth inhibition assay	Inhibition of human GOTO cell growth in a cell viability assay, IC50=5.49576 μM
KYSE-510 cell	Growth inhibition assay	Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50=5.511 μM
NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=5.53278 μM
BFTC-905 cell	Growth inhibition assay	Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.62835 μM
EW-16 cell	Growth inhibition assay	Inhibition of human EW-16 cell growth in a cell viability assay, IC50=5.72093 μM
SK-MEL-30 cell	Growth inhibition assay	Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=5.74543 μM
HLE cell	Growth inhibition assay	Inhibition of human HLE cell growth in a cell viability assay, IC50=5.77489 μM
T98G cell	Growth inhibition assay	Inhibition of human T98G cell growth in a cell viability assay, IC50=5.79635 μM
HUTU-80 cell	Growth inhibition assay	Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=5.84228 μM
NOS-1 cell	Growth inhibition assay	Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=5.94766 μM
SW780 cell	Growth inhibition assay	Inhibition of human SW780 cell growth in a cell viability assay, IC50=5.96949 μM
KYSE-180 cell	Growth inhibition assay	Inhibition of human KYSE-180 cell growth in a cell viability assay, IC50=5.97654 μM
MDA-MB-361 cell	Growth inhibition assay	Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=5.98647 μM
SNU-C2B cell	Growth inhibition assay	Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=6.01138 μM
NCI-H661 cell	Growth inhibition assay	Inhibition of human NCI-H661 cell growth in a cell viability assay, IC50=6.0694 μM
OE33 cell	Growth inhibition assay	Inhibition of human OE33 cell growth in a cell viability assay, IC50=6.14389 μM
TYK-nu cell	Growth inhibition assay	Inhibition of human TYK-nu cell growth in a cell viability assay, IC50=6.21863 μM
COLO-792 cell	Growth inhibition assay	Inhibition of human COLO-792 cell growth in a cell viability assay, IC50=6.25219 μM
HEL cell	Growth inhibition assay	Inhibition of human HEL cell growth in a cell viability assay, IC50=6.2676 μM
D-566MG cell	Growth inhibition assay	Inhibition of human D-566MG cell growth in a cell viability assay, IC50=6.33491 μM
U031 cell	Growth inhibition assay	Inhibition of human U031 cell growth in a cell viability assay, IC50=6.41816 μM
COR-L23 cell	Growth inhibition assay	Inhibition of human COR-L23 cell growth in a cell viability assay, IC50=6.43346 μM
NCI-H2452 cell	Growth inhibition assay	Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=6.52281 μM
BB65-RCC cell	Growth inhibition assay	Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=6.6459 μM
CAL-33 cell	Growth inhibition assay	Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=6.65665 μM
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화학 정보, 보관 및 안정성

분자량	328.41	화학식	C₂₁H₂₀N₄	보관 (수령일로부터)	3년-20°C분말
CAS 번호	881202-45-5	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4

용해도

In vitro
배치:

DMSO : 66 mg/mL (200.96 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 2 mg/mL

Water : Insoluble

DMSO : 66 mg/mL (200.96 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 2 mg/mL

Water : Insoluble

DMSO : 66 mg/mL (200.96 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.
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.	3.300mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 66 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.
Clear solution	5% DMSO 1 95% Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	0.400mg/ml (1.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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.

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	p53 (Cell-free assay) HDM2 (Cell-free assay) Mdm2 (Cell-free assay)
시험관 내(In vitro)	JNJ 26854165는 p53을 활성화하고 HDM2 유비퀴틴 E3 Ligase 길항제로 작용하는 새로운 트립타민 유도체입니다. JNJ 26854165는 OCI-AML-3, MOLM-13, NALM-6 및 REH 세포에 대해 72시간에서 0.24, 0.33, 0.32 및 0.44 μM의 IC50 값으로 백혈병 세포주에서 세포 성장 및 Apoptosis를 억제합니다. 또한, JNJ 26854165는 프로테아솜 매개 p21 분해를 가속화하고 p53에 의한 p21의 전사 유도를 길항합니다. 또한 p53 돌연변이 세포에서 S상 지연을 유도하고 E2F1 발현을 상향 조절하여 S상 세포의 우선적인 Apoptosis를 유도합니다. JNJ 26854165는 Mdm2-p53 복합체와 프로테아솜의 상호작용을 억제하고 Mdm2의 RING 도메인에 결합하여 p53 수치를 증가시킬 수 있는 경구용 Mdm2 억제제입니다. 최근 연구에 따르면 JNJ 26854165는 H460, A549, p53-WT-HCT116 및 p53-null-HCT116의 4가지 인간 암세포주에서 클론 형성 생존을 억제합니다.
생체 내(In vivo)	JNJ 26854165는 20 mg/kg 용량을 경구 투여(매일 5일간, 6주 반복)하여 평가 가능한 고형 종양 이종이식편 36개 중 17개(47%) 및 평가 가능한 ALL 이종이식편 7개 중 5개(71%)에서 EFS 분포에 유의미한 차이를 보였습니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/20406950/ [2] https://pubmed.ncbi.nlm.nih.gov/21937165/ [3] https://pubmed.ncbi.nlm.nih.gov/21922647/ [4] http://0-www.ncbi.nlm.nih.gov.elis.tmu.edu.tw/pubmed/21922647

적용 분야

방법	바이오마커	PMID
Western blot	p53 / HDM2 / HDMX / p21 / Noxa / Puma ABCA1 / ABCG1 / NPC1 / NPC2 / HMGcoR MDM2 / p-MDM2 / p53 Bcr-abl / p-Bcr-abl / p-CrkL / STAT5 / p-STAT5 / STAT3 / p-STAT3	20736344
Growth inhibition assay	Cell viability	23820125
Immunofluorescence	p53	27999193

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT00676910	Completed	Neoplasms	Johnson & Johnson Pharmaceutical Research & Development L.L.C.	November 2006	Phase 1

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