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RG-7112 (RO-5045337)

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InvivoChem Cat #: V0045

CAS #: 939981-39-2Purity ≥98%

Description: RG7112 (also known as RO5045337) is a novel, potent and highly selective antagonist/inhibitor of the p53-MDM2 protein-protein interaction with IC50 of 11 nM. RG-7112 is under clinical development for cancer treatment.

References: Pediatr Blood Cancer. 2013 Apr;60(4):633-41. Exp Hematol. 2014 Feb;42(2):137-45.e5.

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Molecular Weight (MW)	727.78
Formula	C38H48Cl2N4O4S
CAS No.	939981-39-2
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 100 mg/mL (137.7 mM)
	Water:<1 mg/mL (slightly soluble or insoluble)
	Ethanol: N/A
Solubility (In vivo)	1% CMC Na:14 mg/mL
Chemical Name	[(4S,5R)-2-(4-tert-butyl-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethylimidazol-1-yl]-[4-(3-methylsulfonylpropyl)piperazin-1-yl]methanone
Synonym	RG7112; RG-7112; RG 7112; RO5045337; RO 5045337; RO5045337

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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.
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.
Animal model	SJSA-1, SJSA-1luc2, and MHM xenografted Balb/c nude mice
Formulation & Dosage	1% Klucel LF/0.1% Tween 80; 200 mg/kg; oral taken
References	[1]Pediatr Blood Cancer 2013;60:633–641

These protocols are for reference only. InvivoChem does not independently validate these methods.

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