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JNJ-26854165

Cat. No. M2068
JNJ-26854165 Structure
Synonym:

Serdemetan

Size Price Availability Quantity
5mg USD 70  USD70 In stock
10mg USD 110  USD110 In stock
50mg USD 390  USD390 In stock
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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.

Chemical Information
Molecular Weight 328.41
Formula C21H20N4
CAS Number 881202-45-5
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Chargari C, et al. Cancer Lett. Preclinical assessment of JNJ-26854165 (Serdemetan), a novel tryptamine compound with radiosensitizing activity in vitro and in tumor xenografts.

[2] Smith MA, et al. Pediatr Blood Cancer. Initial testing of JNJ-26854165 (Serdemetan) by the pediatric preclinical testing program.

[3] Kojima K, et al. Mol Cancer Ther. The novel tryptamine derivative JNJ-26854165 induces wild-type p53- and E2F1-mediated apoptosis in acute myeloid and lymphoid leukemias.

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


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