GDC-0032

Base Information

Chemical Name:GDC-0032
CAS No.:1282512-48-4
Molecular Formula:C₂₄H₂₈N₈O₂
Molecular Weight:460.539
Hs Code.:
Mol file:1282512-48-4.mol

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

Suppliers and Price of GDC-0032

Supply Marketing:

Business phase:: The product has achieved commercial mass production^*data from LookChem market partment

Manufacturers and distributors:

Manufacture/Brand
Chemicals and raw materials
Packaging
price

TRC
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
100mg
$ 525.00

Matrix Scientific
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 95%
1g
$ 17576.00

DC Chemicals
Taselisib（GDC-0032） >98%
1 g
$ 1600.00

DC Chemicals
Taselisib（GDC-0032） >98%
250 mg
$ 800.00

Crysdot
GDC-0032 98+%
10mg
$ 98.00

Crysdot
GDC-0032 98+%
25mg
$ 179.00

Crysdot
GDC-0032 98+%
50mg
$ 260.00

ChemScene
Taselisib 99.46%
200mg
$ 750.00

ChemScene
Taselisib 99.46%
50mg
$ 250.00

ChemScene
Taselisib 99.46%
100mg
$ 450.00

Total 24 raw suppliers

Chemical Property of GDC-0032

Chemical Property:

Boiling Point:783.3±70.0 °C(Predicted)
PKA:15.54±0.50(Predicted)
PSA：118.67000
Density:1.40±0.1 g/cm3(Predicted)
LogP:3.87450
Solubility.:≥23.05 mg/mL in DMSO; insoluble in H2O; ≥2.79 mg/mL in EtOH with gentle warming

Purity/Quality:

99%, ^*data from raw suppliers

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 ^*data from reagent suppliers

Safty Information:

Pictogram(s):
Hazard Codes:

MSDS Files:

Useful:

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

Technology Process of GDC-0032

There total 29 articles about GDC-0032 which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 90.0%

: 1282513-03-4
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-methylpropanoic acid

: 1282512-48-4
taselisib

Guidance literature:: 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-methylpropanoic acid; With 1,1'-carbonyldiimidazole; In tetrahydrofuran; at 25 ℃; Large scale;

With methanol; ammonia; In tetrahydrofuran; at 25 ℃; for 1h; Large scale;
DOI:10.1021/acs.oprd.9b00050

Reference yield:

: 1282514-64-0
ethyl 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-methylpropanoate

: 1282512-48-4
taselisib

Guidance literature:: Multi-step reaction with 2 steps

1.1: water; lithium hydroxide / methanol / 2 h / 20 °C

1.2: pH 5

2.1: N-ethyl-N,N-diisopropylamine; ammonium chloride; HATU / N,N-dimethyl-formamide / 2 h / 20 °C

With water; ammonium chloride; N-ethyl-N,N-diisopropylamine; HATU; lithium hydroxide; In methanol; N,N-dimethyl-formamide;

Reference yield:

: 1282514-63-9
9-bromo-2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f ]imidazo[1,2-d][1,4]oxazepine

: 1282518-81-3
C₁₃H₂₂BN₃O₃

: 1282512-48-4
taselisib

Guidance literature:: With tetrakis(triphenylphosphine) palladium⁽⁰⁾; potassium acetate; In water; acetonitrile; at 120 ℃; for 0.333333h; Microwave irradiation; Inert atmosphere;
DOI:10.1021/jm4003632