Taselisib (GDC 0032, RG7604) is a potent, next-generation β-subtype PI3K inhibitor that acts on PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, respectively, which is more than 10 times more selective than for PI3kβ.

 

Brand: BCM

 

Target: Carbonic Anhydrase; PI3K

 

Signaling Pathways: Metabolism; PI3K/Akt/mTOR signaling

 

In Vitro: GDC-0032, in combination with fluvestrant, enhances the activity of fluvestrant, resulting in tumor regression and delayed tumor growth (91% tumor growth inhibition (TGI)). In addition,GDC-0032 was combined with tamoxifen to enhance the efficacy of tamoxifen in vivo, and the tumor growth inhibition rate of GDC-0032 was 102%. The pharmacokinetics of GDC-0032 were approximately proportional to dose and independent of time, with an average t1/2 of 40 hours.

 

In Vivo: Preclinical data suggest that GDC-0032 has increased activity in PI3Kα isotype (PIK3CA) mutants and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cell proliferation with an IC50 of 2.5 nM. GDC-0032 is an oral bioavailable, potent, and selective inhibitor of Class I PI3Kα,δ, and γ isoforms with a 30-fold lower inhibition rate against PI3Kβ isoforms compared to PI3Kα isoforms.

 

Boiling Point: 783.3±70.0 °C(Predicted)

 

pKa: 15.54±0.50(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric 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  

 

InChIKey: BEUQXVWXFDOSAQ-UHFFFAOYSA-N  

 

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)

 

Attribute
[Chem Name]	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
[Synonym]	Taselisib; GDC 0032; RG7604
[CAS No.]	1282512-48-4
[MDL No.]	MFCD26142641
[Formula]	C24H28N8O2
[Molecular]	460.53
[Form]	Solid Powder
[Storage]	Sealed in dry, 2-8°C

Goods Tag