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GDC-0152 (RG7419)

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InvivoChem Cat #: V0052

CAS #: 873652-48-3Purity ≥98%

Description: GDC-0152 (RG-7419) is a novel and potent antagonist of IAP (inhibitor of apoptosis) family proteins with antitumor activity. Inhibiting IAPs with Kis of 28 nM, 14 nM, 17 nM and 43 nM for XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 in cell-free assays, respectively; It has lower affinity to cIAP1-BIR2 and cIAP2-BIR2. GDC-0152 is being investigated in Phase 1 clinical trial for cancer treatment.

References: J Med Chem. 2012 May 10;55(9):4101-13.

Related CAS: 873581-21-6 (HCl)

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Molecular Weight (MW)	498.64
Formula	C25H34N6O3S
CAS No.	873652-48-3
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 99 mg/mL (198.5 mM)
	Water: 3 mg/mL (6.0 mM)
	Ethanol: 99 mg/mL (198.5 mM)
Solubility (In vivo)	30% Propylene glycol, 5% Tween 80, 65% D5W: 5mg/mL
Synonym/Chemical Name	GDC0152; RG-7419; GDC0152; RG 7419; GDC 0152; RG7419.; (2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-(4-phenylthiadiazol-5-yl)pyrrolidine-2-carboxamide

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In Vitro	GDC-0152 can block protein−protein interactions that involve IAP proteins and pro-apoptotic molecules. Using transiently transfected HEK293T cells, GDC-0152 is shown to disrupt XIAP binding to partially processed caspase-9 and to disrupt the association of ML-IAP, cIAP1, and cIAP2 with Smac.
In Vivo	GDC-0152 has moderate predicted hepatic clearance based on metabolic stability assays conducted using human liver microsomes. Plasma−protein binding of GDC-0152 is moderate and comparable among mice (88−91%), rats (89−91%), dogs (81−90%), monkeys (76−85%), and humans (75−83%) over the range of concentrations investigated (0.1−100 μM); higher plasma−protein binding is observed in rabbits (95−96%).
Animal model	Human-tumor xenograft mouse models of MDA-MB-231 breast cancer
Formulation & Dosage	phosphate-buffered saline; 10, 50, 100 mg/kg; Oral
References	[1] Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.

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

Purity ≥98%
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NMR

		Flygare JA, et al. J Med Chem, 2012, 55(9), 4101-4113.

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