Basic information Safety Supplier Related

GDC-0032

Basic information Safety Supplier Related

GDC-0032 Basic information

Product Name:
GDC-0032
Synonyms:
  • GDC-0032
  • RG7604/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]-α,α-dimethyl-1H-pyrazole-1-acetamide
  • GDC-0032/(RG-7604)
  • 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
  • Taselisib
  • 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
CAS:
1282512-48-4
MF:
C24H28N8O2
MW:
460.53
Product Categories:
  • Inhibitors
Mol File:
1282512-48-4.mol
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GDC-0032 Chemical Properties

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
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GDC-0032 Usage And Synthesis

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. 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.

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-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

target

PI3Kδ

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.

GDC-0032Supplier

Heze Development Zone chuangli Chemical Co., Ltd. Gold
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+86-530-529 6766,+86-15666160102 15666160102
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info@chuangli-chem.com
Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Email
jkinfo@jkchemical.com
Chembest Research Laboratories Limited
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+86-21-20908456
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sales@BioChemBest.com
Jia Xing Isenchem Co.,Ltd
Tel
0573-85285100 18627885956
Email
isenchem@163.com
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GDC-0032(1282512-48-4)Related Product Information