| Identification | Back Directory | [Name]
GDC-0032 | [CAS]
1282512-48-4 | [Synonyms]
RG-7604
CS-1435
GDC-0032
GDC-3002
Taselisib
RG7604/GDC-0032
GDC-0032/(RG-7604)
Arimoclomol Maleate
Taselisib (GDC-0032)
GDC-0032 (Taselisib)
GDC0032; GDC 0032;RG7604
GDC-0032, TASELISIB; RG-7604
Taselisib - GDC 0032 | RG 7604
GDC-0032, 98%, a potent β-sparing small molecule inhibitor of PI3K
2-(4-(2-(1-Isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxa
GDC-0032 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]-alph
2-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
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
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
1H-Pyrazole-1-acetamide, 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-
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]-alpha,alpha-dimethyl-1H-pyrazole-1-acetamide
GDC-0032 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]-alpha,alpha-dimethyl-1H-pyrazole-1-acetamide | [Molecular Formula]
C24H28N8O2 | [MDL Number]
MFCD26142641 | [MOL File]
1282512-48-4.mol | [Molecular Weight]
460.53 |
| Chemical Properties | Back Directory | [Boiling point ]
783.3±70.0 °C(Predicted) | [density ]
1.40±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥23.05 mg/mL in DMSO; insoluble in H2O; ≥2.79 mg/mL in EtOH with gentle warming | [form ]
solid | [pka]
15.54±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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 | [Uses]
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 is a newly discovered A β-Sparing phosphoinositide 3-kinas
e inhibitor with high unbound exposure and robust in vivo antitumor activity. | [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[1]. The vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice experiencs initial tumor regression after treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.)[2]. | [target]
PI3Kδ | [IC 50]
PI3Kδ: 0.12 nM (Ki); PI3Kα: 0.29 nM (Ki); PI3Kγ: 0.97 nM (Ki); PI3Kβ: 9.1 nM (Ki) | [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. |
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