JNJ-26854165 (Serdemetan)

Description

Biological Activity

Protocol(Only for Reference)

Clinical Trial Information( data from http://clinicaltrials.gov)

Chemical Information

Cell Assay: ^[1]

Animal Study: ^[4]

References

Name: JNJ-26854165 (Serdemetan)
Brand: Selleckchem
SKU: S1172

貨號 Cat. No.: S1172
規格 Size: 5~200mg
品牌 Brand: Selleckchem

JNJ-26854165 (Serdemetan)

Catalog No.S1172

JNJ-26854165 acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.

Size

Price

Stock

Quantity

10mM/1mLIn DMSO	USD 176	In stock	0 1 2 3 4 5 6 7 8 9 10
5mg	USD 138	In stock	0 1 2 3 4 5 6 7 8 9 10
25mg	USD 466	In stock	0 1 2 3 4 5 6 7 8 9 10
100mg	USD 1222	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Cell lines	OCI-AML-3, MOLM-13, NB4 and U937 cells
Concentrations	0-10 μM
Incubation Time	72 hours
Method	Cell lines are maintained in RPMI 1640 medium containing 10% heat-inactivated fetal calf serum (FCS). OCI-AML-3, MOLM-13, NB4 and U937 cells are derived from acute myelogenous leukemia (AML) patients, K562 from a chronic myelogenous leukemia (CML) patient in blast crisis, and NALM-6, REH, P12-ICHIK

Animal Models	CB17SC scid^-/- female mice.
Dosages	≤20 mg/kg
Administration	Administered via p.o.
Solubility	1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT00676910	Completed	Neoplasms	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	2006-11	Phase 1

Description

JNJ-26854165 acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.

In vitro

JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells. ^[1] JNJ 26854165 is an oral Mdm2 inhibitor which can inhibit the interaction of Mdm2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of Mdm2. ^[2] A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116. ^[3]

JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks. ^[4]

Download JNJ-26854165 (Serdemetan) SDF

Molecular Weight (MW)	328.41
Formula	C₂₁H₂₀N₄
CAS No.	881202-45-5

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	66 mg/mL (200 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	2 mg/mL (6 mM)
	In vivo	1% DMSO/30% polyethylene glycol/1% Tween 80,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.