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Inavolisib

Catalog No. T15375 CAS 2060571-02-8

Synonyms: GDC-0077, RG6114

Inavolisib (GDC-0077) is an orally available and selective inhibitor of PI3Kα (IC50=0.038 nM). Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3.

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Inavolisib, CAS 2060571-02-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 203.00
5 mg	In stock	$ 413.00
10 mg	In stock	$ 675.00
25 mg	In stock	$ 973.00
50 mg	In stock	$ 1,430.00
100 mg	In stock	$ 1,930.00
200 mg	In stock	$ 2,590.00
500 mg	In stock	$ 3,870.00
1 mL * 10 mM (in DMSO)	In stock	$ 425.00

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Purity: 99.74%

Purity: 99.41%

Purity: 98.84%

Purity: 98.51%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Inavolisib (GDC-0077) is an orally available and selective inhibitor of PI3Kα (IC50=0.038 nM). Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3.
Targets&IC50	PI3Kα:0.038 nM
In vitro	Inavolisib is >300-fold more selective for PI3Kα over the other class I PI3K isoforms (β, δ, and γ). Inavolisib is >2000-fold more selective over PIK family members. Inavolisib selectively degrades mutant PI3Kα in a proteasome-dependent fashion. When compared to PIK3CA wild-type cells, Inavolisib results in a reduction of PI3K pathway activity biomarkers such as pAKT and pPRAS40, inhibition of cell proliferation. Inavolisib also increased apoptosis in human PIK3CA-mutant breast cancer cell lines to a greater extent [1].
In vivo	In patient-derived PIK3CA-mutant breast cancer xenograft models, Inavolisib (p.o.) causes tumor regressions, induction of apoptosis, and a reduction of pAKT, pPRAS40, and pS6RP in a dose-dependent fashion [1].

Synonyms	GDC-0077, RG6114
Molecular Weight	407.37
Formula	C18H19F2N5O4
CAS No.	2060571-02-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (245.48 mM), Sonication is recommended.

References and Literature

1. R Hong, Abstract PD4-14: GDC-0077 is a selective PI3Kalpha inhibitor that demonstrates robust efficacy in PIK3CA mutant breast cancer models as a single agent and in combination with standard of care therapies. 2017 San Antonio Breast Cancer Symposium. 2. Hanan EJ, et al. Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα. J Med Chem. 2022 Dec 22;65(24):16589-16621. 3. Song KW, et al. RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy. Cancer Discov. 2022 Jan;12(1):204-219.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Neuronal Differentiation Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Neural Regeneration Compound Library Anti-Cancer Compound Library

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Keywords

Inavolisib 2060571-02-8 Apoptosis PI3K/Akt/mTOR signaling PI3K GDC-0077 GDC0077 Phosphoinositide 3-kinase Inhibitor RG6114 RG-6114 GDC 0077 inhibit RG 6114 inhibitor

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