| In Vitro | RG7112 has been profiled extensively in many cell lines. In 15 cancer cell lines expressing wild-type p53, it shows IC50 in the range of 0.18 - 2.2 μM. However, the inhibition is much less in seven cancer cell lines with p53 mutation, IC50 5.7 - 20.3 μM. The overall selectivity is 14-fold. |
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| In Vivo | In the SJSA1 xenograft mouse model, RG7112 (200 mg/kg, p.o.) penetrates tumor cells and activate p53 and its 2 major functions, cell-cycle arrest and apoptosis. In nude mice bearing SJSA-1, and MHMn xenografts, RG7112 (100 mg/kg, p.o.) causes tumor regression. In rats, RG7112 impairs thrombopoiesis via activation of p53. |
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| Animal model | SJSA-1, SJSA-1luc2, and MHM xenografted Balb/c nude mice |
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| Formulation & Dosage | 1% Klucel LF/0.1% Tween 80; 200 mg/kg; oral taken |
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| References | [1]Pediatr Blood Cancer 2013;60:633–641 |
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