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GDC-0032

CAT: 0013-GTR19163929-02Size: 2 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163929-02Size:2 mg
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Description
GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. (In Vitro) :Taselisib (GDC-0032) (100 nM) inhibits AKT/mTOR signaling in PIK3CA mutant cell lines but not in cells with loss or mutation of PTEN; Taselisib (GDC-0032) enhances radiation-induced apoptosis and inhibits growth in head and neck cancer cell lines that are sensitive to its single-agent activiy. Taselisib (GDC-0032) enhances the effects of MEK1/2 inhibition on both BRAFV600E/PTENNull human melanoma cells autochthonous mouse melanomas. (In Vivo) :Taselisib (GDC-0032) (5 mg/kg, p.o.) potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy; Taselisib (GDC-0032) and radiation is more effective than either treatment alone in nude mice implanted with subcutaneous Cal-33 xenografts. The vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice experiencs initial tumor regression after treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.) .
CAS Number
1282512-48-4
Product Name Alternative
?Taselisib
Purity
>98% (HPLC)
Solubility
Ethanol: 7 mg/mL warmed (15.19 mM) ; DMSO: 70 mg/mL warmed (151.99 mM)
Smiles
CC (C) (N1N=CC (C2=CC=C3C4=NC (C5=NC (C) =NN5C (C) C) =CN4CCOC3=C2) =C1) C (N) =O
Molecular Formula
C24H28N8O2
Molecular Weight
460.53
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2- (4- (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

Chemical Information

Taselisib

Taselisib has been used in trials studying the treatment and basic science of LYMPHOMA, Breast Cancer, Ovarian Cancer, Solid Neoplasm, and HER2/Neu Negative, among others.

CAS Number1282512-48-4
PubChem CID51001932
IUPAC 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
Molecular FormulaC24H28N8O2
Molecular Weight460.5
XLogP1.8
Topological Polar Surface Area119
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count6
Rotatable Bond Count5
Heavy Atom Count34
Formal Charge0
Complexity750
SMILES
CC1=NN(C(=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)C5=CN(N=C5)C(C)(C)C(=O)N)C(C)C
InChI
InChI=1S/C24H28N8O2/c1-14(2)32-22(27-15(3)29-32)19-13-30-8-9-34-20-10-16(6-7-18(20)21(30)28-19)17-11-26-31(12-17)24(4,5)23(25)33/h6-7,10-14H,8-9H2,1-5H3,(H2,25,33)
InChIKey
BEUQXVWXFDOSAQ-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Taselisib
CAS: 1282512-48-4
CID: 51001932
Formula: C24H28N8O2
MW: 460.5
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight460.5
XLogP31.8
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count6
Rotatable Bond Count5
Exact Mass460.23352217
Monoisotopic Mass460.23352217
Topological Polar Surface Area119 Ų
Heavy Atom Count34
Formal Charge0
Complexity750
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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Alternative Products

CatalogName
B1047-5GDC-0032
BG166285-01GDC 0032
A12831-50GDC-0032 50mg
C12444-1gTaselisib (GDC 0032)
MBS384745-01GDC-0032 (Taselisib)
A12831-25GDC-0032 25mg
A12831-10GDC-0032 10mg
A12831-5GDC-0032 5mg

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