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Cat. No. M2068
JNJ-26854165 Structure


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Biological Activity

JNJ-26854165 (Serdemetan) is a p53-activating agent with antiproliferative activity in various p53 wild-type (WT) tumor cell lines. JNJ-26854165 inhibited clonogenic survival in all cell lines, but in a lower extent in p53-null-HCT116. JNJ-26854165 also inhibited proliferation, capillary tube formation and migration of HMEC-1 cells. JNJ-26854165 demonstrated cytotoxic activity in vitro. In vivo, JNJ-26854165 (Serdemetan) caused a greater than additive increase in tumor growth delay. JNJ-26854165 induced significant differences in EFS distribution compared to control in 18 of 37 solid tumors and in 5 of 7 of the evaluable ALL xenografts in vivo. JNJ-26854165 (Serdemetan) treatment at 0.25μM in H460 and at 5μM in A549 cells resulted in a sensitivity-enhancement ratio of 1.18 and 1.36, respectively. JNJ-26854165 treatment induced 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. JNJ-26854165 accelerated the proteasome-mediated degradation of p21 and antagonized the transcriptional induction of p21 by p53. JNJ-26854165 is currently being evaluated in Phase I clinical trials.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 328.41
Formula C21H20N4
CAS Number 881202-45-5
Purity 99.20%
Solubility DMSO 60 mg/mL
Storage at -20°C

Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts.
Chargari C, et al. Cancer Lett. 2011 Dec 22;312(2):209-18. PMID: 21937165.

Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program.
Smith MA, et al. Pediatr Blood Cancer. 2012 Aug;59(2):329-32. PMID: 21922647.

The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias.
Kojima K, et al. Mol Cancer Ther. 2010 Sep;9(9):2545-57. PMID: 20736344.

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Keywords: JNJ-26854165, Serdemetan supplier, p53, inhibitors

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