For research use only. Not for therapeutic Use.
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Taselisib(cas 1282512-48-4), also known as GDC-0032, is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.<br />
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<span>Taselisib</span> is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ isoforms, with 30 fold less inhibition of the PI3K β isoform relative to the PI3Kα isoform. Preclinical data show that GDC-0032 has increased activity against PI3Kα isoform (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM. GDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t1/2 of 40 hours. The combination of GDC-0032 enhances activity of fulvestrant resulting in tumor regressions and tumor growth delay (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 with tamoxifen enhances the efficacy of tamoxifen in vivo (102%TGI for GDC-0032).
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| Catalog Number | I001112 |
| CAS Number | 1282512-48-4 |
| Synonyms | GDC-0032 |
| Molecular Formula | C₂₄H₂₈N₈O₂ |
| Purity | ≥95% |
| Target | PI3K |
| Solubility | 10 mM in DMSO |
| Storage | 3 years -20C powder |
| IC50 | 0.29 nM/0.12 nM /0.97 nM(PI3Kα/δ/γ) [1] |
| 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) |
| InChIKey | BEUQXVWXFDOSAQ-UHFFFAOYSA-N |
| 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 |
| Reference | 1: Zumsteg ZS, Morse N, Krigsfeld G, Gupta G, Higginson DS, Lee NY, Morris L, 2: Hoeflich KP, Guan J, Edgar KA, O/’Brien C, Savage H, Wilson TR, Neve RM, 3: Juric D, Krop I, Ramanathan RK, Wilson TR, Ware JA, Sanabria Bohorquez SM, </br> 5: Ding X, Faber K, Shi Y, McKnight J, Dorshorst D, Ware JA, Dean B. Validation </br> |
