Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie

GDC-0152 [873652-48-3]

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Katalog-Nummer NB-64-33514-10mg

Size : 10mg

Marke : Neo Biotech

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GDC-0152

(Synonyms: GDC0152) Copy Product Info

Synonyms: GDC0152

Catalog No. T6299 Copy Product Info

Purity: 99.32%

GDC-0152 is a potent inhibitor of IAPs.

Cas No. 873652-48-3

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.32%

Color:White

Product Introduction

Bioactivity

Description	GDC-0152 is a potent inhibitor of IAPs.
Targets & IC50	MLXBIR3SG:14 nM(Ki), XIAP BIR3:28 nM(Ki), XIAP BIR2:112 nM(Ki), CIAP2-BIR3:43 nM(Ki), CIAP1-BIR3:17 nM(Ki)
In vitro	GDC-0152 inhibits protein−protein interactions between IAP proteins and pro-apoptotic molecules. It disrupts XIAP's binding to caspase-9 and the association of ML-IAP, cIAP1, and cIAP2 with Smac in transiently transfected HEK293T cells. Similarly, in melanoma SK-MEL28 cells, GDC-0152 abolishes the natural association between ML-IAP and Smac. It decreases cell viability in the MDA-MB-231 breast cancer cell line without affecting normal human mammary epithelial cells (HMEC). Furthermore, GDC-0152 activates caspases 3 and 7 dependent on dose and time, and induces rapid degradation of cIAP1 in A2058 melanoma cells at low concentrations, aligning with its affinity for cIAP1.
In vivo	GDC-0152 exhibits moderate hepatic clearance as inferred from metabolic stability assays using human liver microsomes, with its plasma-protein binding being moderate yet consistent across several species, including mice (88−91%), rats (89−91%), dogs (81−90%), monkeys (76−85%), and humans (75−83%) across investigated concentrations (0.1−100 μM); however, rabbits show higher plasma-protein binding rates (95−96%). Importantly, GDC-0152 does not show a preference for red blood cell distribution, as evidenced by blood-plasma partition ratios ranging from 0.6 to 1.1 across all tested species. Pharmacokinetic profiles reveal a maximum concentration (C max) of 53.7 μM and an area under the curve (AUC) of 203.5 h·μM. [1]
Synonyms	GDC0152
Kinase Assay	Fluorescence polarization-based competition assay: Inhibition constants ( Ki ) for the antagonists are determined by addition of the IAP protein constructs to wells containing serial dilutions of the antagonists or the peptide AVPW, and the Hid-FAM probe or AVP-diPhe-FAM probe, as appropriate, in the polarization buffer. Samples are read after a 30-minute incubation. Fluorescence polarization values are plotted as a function of the antagonist concentration, and the IC50 values are obtained by fitting the data to a 4-parameter equation using software. Ki values for the antagonists are determined from the IC50 valued.
Cell Research	MDA-MB-231 breast carcinoma cells and HMECs are treated with the indicated concentrations of GDC-0152. Cell death is assessed using the CellTiter-Glo luminescent cell viability assay 72 h following the start of treatment.(Only for Reference)

Chemical Properties

Molecular Weight	498.64
Formula	C₂₅H₃₄N₆O₃S
Cas No.	873652-48-3
Smiles	C([C@@H](NC([C@@H](NC)C)=O)[C@@H]1CCCCC1)(=O)N2[C@H](C(NC3=C(N=NS3)C4=CC=CC=C4)=O)CCC2
Relative Density.	no data available

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 92 mg/mL (184.5 mM), Sonication is recommended.

Ethanol: 92 mg/mL (184.5 mM), Sonication is recommended.

H2O: 3 mg/mL (6.02 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.62 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.0055 mL	10.0273 mL	20.0545 mL	100.2727 mL
5 mM	0.4011 mL	2.0055 mL	4.0109 mL	20.0545 mL

DMSO/Ethanol

	1mg	5mg	10mg	50mg
10 mM	0.2005 mL	1.0027 mL	2.0055 mL	10.0273 mL
20 mM	0.1003 mL	0.5014 mL	1.0027 mL	5.0136 mL
50 mM	0.0401 mL	0.2005 mL	0.4011 mL	2.0055 mL
100 mM	0.0201 mL	0.1003 mL	0.2005 mL	1.0027 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

XIAP-BIR3XIAP-BIR2MLXBIR3SGInhibitorinhibitIAPGDC-0152GDC 0152cIAP2-BIR3cIAP1-BIR3

Related Tags: GDC-0152 chemical structure | GDC-0152 in vivo | GDC-0152 in vitro | GDC-0152 formula | GDC-0152 molecular weight