A potent PI3K inhibitor that is β-sparing
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GDC-0032

Item No. 17387

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[5,6-dihydro-2-[3-methyl-1-(1-methylethyl)-1H-1,2,4-triazol-5-yl]imidazo[1,2-d][1,4]benzoxazepin-9-yl]-α,α-dimethyl-1H-pyrazole-1-acetamide
CAS Number
1282512-48-4
Synonyms
  • Taselisib
Molecular Formula
C24H28N8O2
Formula Weight
460.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 70 mg/mLEthanol: <1 mg/mLWater: <1 mg/mL
λmax
217, 301, 321 nm
SMILES
CC1=NN(C(C)C)C(C2=CN(CCO3)C(C4=C3C=C(C5=CN(C(C)(C)C(N)=O)N=C5)C=C4)=N2)=N1
InChi Code
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)
InChi Key
BEUQXVWXFDOSAQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $178

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    Product Description

    GDC-0032 is a potent inhibitor of phosphatidylinositol 3-kinase (PI3K) isoforms α, δ, and γ (IC50s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ.1 It is over 1,000-fold selective for p100α over other PI3K-like kinases, including DNA-dependent protein kinase catalytic subunits, ATM, and ATR. GDC-0032 has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo, suppressing the growth of tumors in a mouse xenograft model at low drug dose levels.2,1,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ndubaku, C.O., Heffron, T.P., Staben, S.T., et al. 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. 56(11), 4597-45610 (2013).

    2. Lopez, S., Schwab, C.L., Cocco, E., et al. Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo. Gynecol. Oncol. 135(2), 312-317 (2014).

    3. Zumsteg, Z.S., Morse, S., Krigsfeld, G., et al. Taselisib (GDC-0032), a potent β-sparing small molecule inhibitor of PI3K, radiosensitizes head and neck squamous carcinomas containing activating PIK3CA alterations. Clin. Cancer Res. 22(8), 2009-2019 (2016).

    Product Citations

    Small, J.C., Joblin-Mills, A., Carbone, K., et al. Phenotypic screening for small molecules that protect b-cells from glucolipotoxicity. ACS Chem. Biol. 17(5), 1131-1142 (2022).