|N1-(2-(1H-吲哚-3-基)乙基)-N4-(吡啶-4-基)苯-1,4-二胺|CsnPharm

CAS No.: 881202-45-5

Serdemetan Catalog No. CSN13427

Synonyms: JNJ-26854165

Serdemetan acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, and inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.

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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JNJ-26854165 is a p53-activating agent which can induce p53-mediated apoptosis in acute leukemia cells with wild-type p53, in which p53 rapidly drives transcription-independent apoptosis followed by activation of a transcription-dependent pathway. It accelerated the proteasome-mediated degradation of p21 and antagonized the transcriptional induction of p21 by p53^[3]. The action of JNJ-26854165 relies on HDM2, a key regulator of p53, mediating its rapid degradation. It is regarded as a first-in-class HDM2-inhibitor in phase I development^[2].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
5637 cell	-	Growth inhibition assay	-	Inhibition of human 5637 cell growth in a cell viability assay, IC50=4.79652 μM	SANGER
769-P cell	-	Growth inhibition assay	-	Inhibition of human 769-P cell growth in a cell viability assay, IC50=1.82224 μM	SANGER
786-0 cell	-	Growth inhibition assay	-	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.72989 μM	SANGER

更多
动物研究
剂量
Mice: 20 mg/kg^[3] (p.o.), 50 mg/kg^[4] (p.o.)

给药途径
p.o.
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT00676910 Neoplasms Phase 1 Completed - -
参考文献

动物研究
剂量	Mice: 20 mg/kg^[3] (p.o.), 50 mg/kg^[4] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00676910	Neoplasms	Phase 1	Completed	-	-

[1] Kojima K, Burks JK, et al. The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias. Mol Cancer Ther. 2010 Sep;9(9):2545-57.
[2] A first-in-class HDM2-inhibitor (JNJ-26854165) in phase I development shows potent activity against multiple myeloma (MM) cells in vitro and ex vivo
[3] Kojima K, Burks JK, Arts J, Andreeff M. The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias. Mol Cancer Ther. 2010 Sep;9(9):2545-57. doi: 10.1158/1535-7163.MCT-10-0337. Epub 2010 Aug 24. PMID: 20736344; PMCID: PMC2949269.

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
- 3.0450 mL
- 15.2249 mL
- 30.4497 mL
- 5 mM
- 0.6090 mL
- 3.0450 mL
- 6.0899 mL
- 10 mM
- 0.3045 mL
- 1.5225 mL
- 3.0450 mL

技术信息

CAS号	881202-45-5	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C21H20N4	运输	蓝冰
分子量	328.41	别名	JNJ-26854165

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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

Serdemetan Catalog No. CSN13427

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