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Chemical Structure| 2060571-02-8 Chemical Structure| 2060571-02-8

Structure of Inavolisib
CAS No.: 2060571-02-8

Chemical Structure| 2060571-02-8

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Inavolisib is an orally active selective PI3Kδ inhibitor that effectively regulates the PI3K signaling pathway, suitable for treating immune system-related cancers and inflammatory diseases.

Synonyms: GDC 0077; RG6114; RO-7113755

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of Inavolisib

CAS No. :2060571-02-8
Formula : C18H19F2N5O4
M.W : 407.37
SMILES Code : C[C@H](NC1=CC=C2C3=NC(N4C(OC[C@H]4C(F)F)=O)=CN3CCOC2=C1)C(N)=O
Synonyms :
GDC 0077; RG6114; RO-7113755
English Name :(S)-2-((2-((S)-4-(Difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide
MDL No. :MFCD31382124

Safety of Inavolisib

Related Pathways of Inavolisib

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110α

    PI3K alpha, IC50:0.038 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
SK-BR-3 or HCC1569 cells 2 µM 24 hours To assess the effects of PI3K inhibitors on the proliferation of HCC1569 cells. Results showed that HCC1569 cells were less susceptible to inavolisib than SK-BR-3 cells. Cancer Metab. 2025 Feb 7;13(1):6.
MCF-7 cells 0.12 µM and above 4 days To assess the cytotoxic response of GDC-0077 in PIK3CAE545K-mutant MCF7 cells. Results showed a strong cytotoxic response at concentrations of 0.12 μmol/L and above. Cancer Discov. 2022 Jan;12(1):204-219.
HCC1954 cells 1 µM 8 hours To assess the effect of taselisib on p110a protein depletion in PIK3CAH1047R-mutant HCC1954 cells. Results showed dose-dependent depletion of p110a protein. Cancer Discov. 2022 Jan;12(1):204-219.
MCF7 PIK3CA E545K 0.123 µM Evaluate the effect of GDC-0077 in combination with palbociclib Cancer Discov. 2022 Jan;12(1):204-219.
HCC1954 PIK3CA H1047R 0.5 µM 24 h Assess the effect of GDC-0077 on p110a protein levels Cancer Discov. 2022 Jan;12(1):204-219.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice MCF7 orthotopic xenograft model Oral 25 mg/kg Once daily for 28 days To evaluate the antitumor effect of inavolisib in combination with vepdegestrant. The results showed that the combination induced tumor regression in the MCF7 xenograft model. Clin Cancer Res. 2024 Aug 15;30(16):3549-3563.
NCR nude mice HCC1954 xenograft model Oral 50 mg/kg Single dose To assess the efficacy of GDC-0077 in depleting p110a protein in HCC1954 xenograft model. Results showed p110a protein depletion for up to 8 hours. Cancer Discov. 2022 Jan;12(1):204-219.
Mice HCC1954 PIK3CA H1047R xenograft model Oral 50 mg/kg Once daily Evaluate the antitumor efficacy of GDC-0077 in vivo Cancer Discov. 2022 Jan;12(1):204-219.
Mice MCF7 orthotopic xenograft model Oral 25 mg/kg Once daily for 5 days, 2 days off, repeated 4 times Inavolisib in combination with vepdegestrant showed antitumor activity in the MCF7 xenograft model, leading to tumor volume reduction. Clin Cancer Res. 2024 Aug 15;30(16):3549-3563

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.27mL

2.45mL

1.23mL

24.55mL

4.91mL

2.45mL

 

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