Taselisib - CAS 1282512-48-4
Catalog number: 1282512-48-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C24H28N8O2
Molecular Weight:
460.542
COA:
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Targets:
PI3K
Description:
Taselisib, also known as GDC0032 or RG7606, is a selective, potent, orally bioavailable inhibitor of PI3Ka with a Ki = 0.2nM, and with reduced inhibitory activity against PI3K. This selectivity profile, and excellent pharmacokinetic and pharmaceutical properties, allowed for greater efficacy in vivo at the maximum tolerated dose relative to a pan Class I PI3K inhibitor in PIK3CA mutant xenografts. Notably, GDC-0032 preferentially inhibited PIK3CA mutant cells relative to cells with wild-type PI3K. GDC-0032 potently inhibits signal transduction downstream of PI3K and induces apoptosis at low concentrations in breast cancer cell lines and xenograft models that harbor PIK3CA mutations.
Appearance:
solid powder
Synonyms:
GDC-0032; GDC0032; GDC 0032; RG7604; RG-7604; RG 7604; Taselisib.
MSDS:
Inquire
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)
Canonical 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
Current Developer:
Genentech.
1.Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations.
Zumsteg ZS1, Morse N2, Krigsfeld G3, Gupta G4, Higginson DS5, Lee NY5, Morris L2, Ganly I2, Shiao SL6, Powell SN5, Chung CH3, Scaltriti M2, Baselga J7. Clin Cancer Res. 2016 Apr 15;22(8):2009-19. doi: 10.1158/1078-0432.CCR-15-2245. Epub 2015 Nov 20.
PURPOSE: ActivatingPIK3CAgenomic alterations are frequent in head and neck squamous cell carcinoma (HNSCC), and there is an association between phosphoinositide 3-kinase (PI3K) signaling and radioresistance. Hence, we investigated the therapeutic efficacy of inhibiting PI3K with GDC-0032, a PI3K inhibitor with potent activity against p110α, in combination with radiation in HNSCC.
2.Taselisib, a selective inhibitor of PIK3CA, is highly effective on PIK3CA-mutated and HER2/neu amplified uterine serous carcinoma in vitro and in vivo.
Lopez S1, Schwab CL2, Cocco E2, Bellone S2, Bonazzoli E2, English DP2, Schwartz PE2, Rutherford T2, Angioli R1, Santin AD3. Gynecol Oncol. 2014 Nov;135(2):312-7. doi: 10.1016/j.ygyno.2014.08.024. Epub 2014 Aug 27.
OBJECTIVE: To evaluate the efficacy of taselisib, a selective inhibitor of PIK3CA, against primary uterine serous carcinomas (USC) harboring PIK3CA mutations and HER2/neu gene amplification.
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CAS 1282512-48-4 Taselisib

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