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GDC-0032

Catalog No.
B1047
PI3Kα inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$96.00
In stock
5mg
$74.00
In stock
10mg
$110.00
In stock
25mg
$233.00
In stock
100mg
$566.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

GDC-0032 is a novel and potent benzoxepin inhibitor of PI3Kα isoform with the Ki value of 0.29nM for PI3Kα[1].

GDC-0032 has been reported to potently inhibit PI3Kα and have the selectivity over other PI3Ks with the IC50 values of 0.29nM, 0.91nM and 0.97nM for PI3Kα, PI3Kβ and PI3Kγ, respectively. In addition, GDC-0032 has been revealed to suppress the proliferative cellular activity with the EC50 value of 25nM and 571nM in MCF7 cells and PC3 cells, respectively. The IC50 values of GDC-0032 inhibiting cell activity are 4nM and 31nM in MCF7 cells and PC3 cells, respectively. In vivo, GDC-0032 has shown the inhibition of growth in MCF7-neo/Her2 xenograft model grown in nude mice [1].

References:
[1] Ndubaku CO1, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt460.53
Cas No.1282512-48-4
FormulaC24H28N8O2
Solubility≥23.05 mg/mL in DMSO; insoluble in H2O; ≥2.79 mg/mL in EtOH with gentle warming
Chemical Name2-methyl-2-[4-[2-(5-methyl-2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]propanamide
SDFDownload SDF
Canonical SMILESCC1=NN(C(=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)C5=CN(N=C5)C(C)(C)C(=O)N)C(C)C
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

MCF7-neo/HER2 cells

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

2.5 nM

Applications

In MCF7-neo/HER2 cells, GDC-0032 inhibited cell proliferation with an IC50 value of 2.5 nM.

Animal experiment [1]:

Animal models

MCF7-neo/Her2 xenograft model

Dosage form

1.4, 2.8, 5.8, 11.25 or 22.5 mg/kg; p.o.; q.d., for 20 days

Applications

GDC-0032 dose-dependently increased TGI and tumor regressions. In addition, GDC-0032 was well-tolerated with less than 10% body weight loss observed when compared with the vehicle group.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Ndubaku CO1, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56(11):4597-610.

Biological Activity

Description GDC-0032 is a potent, next-generation inhibitor of β isoform-sparing PI3K with IC50 values of 0.29 nM/0.12 nM/0.97nM for PI3Kα/δ/γ, respectively.
Targets PI3Kδ PI3Kα PI3Kγ      
IC50 0.12 nM 0.29 nM 0.97nM      

Quality Control

Chemical structure

GDC-0032