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APR-246

Chemical Structure : APR-246

CAS No.: 5291-32-7

APR-246 (Eprenetapopt, PRIMA-1MET, APR246)

Catalog No.: PC-62406Not For Human Use, Lab Use Only.

APR-246 (Eprenetapopt, PRIMA-1MET) is a methylated derivative of PRIMA-1 that restores mutant p53 activity, acts synergistically with chemotherapeutic agents to inhibit tumor cell proliferation.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

APR-246 (Eprenetapopt, PRIMA-1MET) is a methylated derivative of PRIMA-1 that restores mutant p53 activity, acts synergistically with chemotherapeutic agents to inhibit tumor cell proliferation.
APR-246 (Eprenetapopt, PRIMA-1MET) also restores the pro-apoptotic function to mutant TAp63γ and TAp73β in tumor cells but has less effect on TAp73α.
APR-246 (Eprenetapopt, PRIMA-1MET) induces mutant p53-dependent mitochondria-mediated apoptosis through activation of caspase-2 with subsequent cytochrome c release and further activation of downstream caspase-9 and caspase-3.
APR-246 (Eprenetapopt, PRIMA-1MET) inhibits tumor xenograft growth in vivo.

Physicochemical Properties

M.Wt 199.25
Formula C10H17NO3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(Hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one

References

1. Shen J, et al. Oncogene. 2008 Nov 20;27(51):6571-80.

2. Bykov VJ, et al. Oncogene. 2005 May 12;24(21):3484-91.

3. Rökaeus N, et al. Oncogene. 2010 Dec 9;29(49):6442-51.

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