GLPBio

GDC-0077 (RG6114)

Catalog No.: GC32710Purity:>99.00%Synonyms: GDC-0077; RG6114
COASDSData Sheet
GDC-0077 (RG6114) is a potent and selective PI3Kα inhibitor with an IC50 of 0.038nM.

Products are for research use only. Not for human use. We do not sell to patients.

GDC-0077 (RG6114)
Cas No.: 2060571-02-8
10mM (in 1mL DMSO)In Stock
$333.00
1
1mgIn Stock
$158.00
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5mgIn Stock
$373.00
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10mgIn Stock
$526.00
1
25mgIn Stock
$783.00
1
50mgIn Stock
$1,070.00
1
100mgIn Stock
$1,450.00
1
200mgIn Stock
$1,950.00
1
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Description

GDC-0077 (RG6114) is a potent and selective PI3Kα inhibitor with an IC50 of 0.038nM. GDC-0077 is > 300-fold more selective for PI3Kα over the other class I PI3K isoforms (β, δ, and γ) and > 2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3[1]. GDC-0077 achieves precise targeting of PIK3CA-mutated tumors through a dual-action mechanism: selectively inhibiting PI3Kα activity and inducing the degradation of mutant p110α protein[2]. GDC-0077 is commonly used in the study of breast cancer.

GDC-0077 (0.3μM, 2 to 3 weeks) significantly inhibited proliferation in PIK3CA-mutant cell lines compared to the control. GDC-0077 combined with cobimetinib showed an increased cytotoxic response in four of five colorectal cancer cell lines[3].

GDC-0077 (25mg/kg/day, 25 days, i.g.) markedly enhanced the antitumor efficacy of the palbociclib-fulvestrant combination, elevating the mean tumor growth inhibition (TGI) from 71% to 106%[4].

References:
[1] Hong R, Edgar K, Song K, et al. 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[J]. Cancer research, 2018, 78(4_Supplement): PD4-14-PD4-14.
[2] Zhu R, Zhang H, Zhang F. Mechanistic optimization of inavolisib combined with CDK4/6 inhibitors in the treatment of PIK3CA-mutated breast tumors[J]. Frontiers in Immunology, 2025, 16: 1693927.
[3] Song K W, Ong C C, Lin E, et al. KRAS codon-specific mutations differentially toggle PI3K pathway signaling and alter sensitivity to inavolisib (GDC-0077)[J]. Molecular Cancer Therapeutics, 2025, 24(12): 1890-1901.
[4] Song K W, Edgar K A, Hanan E J, et al. RTK-dependent inducible degradation of mutant PI3Kα drives GDC-0077 (Inavolisib) efficacy[J]. Cancer discovery, 2022, 12(1): 204-219.

Protocol

Cell experiment [1]:

Cell lines

PIK3CA-mutant cell lines

Preparation Method

Twelve-well plates were seeded with 10,000 to 20,000 cells/well in a volume of 1mL and incubated at 37°C under 5% CO2 for 24 hours. Compounds (DMSO, 0.3μM GDC-0077, 0.3μM cobimetinib, or a combination of the two drugs) were added the next day at indicated concentration for 2 to 3 weeks. The medium was replaced weekly with fresh medium containing the drugs. Then the medium was aspirated and 100μL of 0.5% crystal violet was added for 15 minutes. The dye was discarded and the cells were washed with PBS for 5 to 10 minutes five times. PBS was then aspirated and the cells were imaged using GelCount.

Reaction Conditions

0.3μM, 2 to 3 weeks

Applications

GDC-0077 significantly inhibited proliferation in PIK3CA-mutant cell lines compared to the control.
Animal experiment [2]:

Animal models

PIK3CA-mutated breast cancer mouse model

Preparation Method

HCC1954 tumor cells (5×106) were inoculated in the 2/3 mammary fat pads of female NCR nude mice, whereas WHIM20 and HCI-003 tumors (50mm3) were engrafted in 2/3 mammary fat pads in female NOD-SCID gamma mice. Tumor Volume (mm3) = (Length × Width2) × 0.5. Mice for efficacy studies were distributed into 8 to 10 mice/group with a mean tumor volume of 200 to 250mm3 at the initiation of dosing. Tumor growth inhibition as a percentage of vehicle control (%TGI) was calculated as the percentage of the AUC (Area Under the Curve) for the respective dose group per day in relation to the vehicle, using the following formula: %TGI = 100 × (1 – AUCdose/AUCvehicle). The PI3K inhibitors taselisib, GDC-0941, GDC-0077, and BYL719 were formulated in methylcellulose Tween vehicle consisting of 0.5% (w/v) methylcellulose, 0.2% (w/v) polysorbate 80 (Tween-80) and dosed orally by gavage daily. Tumor sizes and mouse body weights were recorded twice weekly, and mice with tumor volume exceeding 2,000mm3 or body weight loss of 20% of starting weight were promptly euthanized.

Dosage form

25mg/kg/day, 25 days, i.g.

Applications

GDC-0077 markedly enhanced the antitumor efficacy of the palbociclib-fulvestrant combination, elevating the mean tumor growth inhibition (TGI) from 71% to 106%.

References:
[1] Song K W, Ong C C, Lin E, et al. KRAS codon-specific mutations differentially toggle PI3K pathway signaling and alter sensitivity to inavolisib (GDC-0077)[J]. Molecular Cancer Therapeutics, 2025, 24(12): 1890-1901.
[2] Song K W, Edgar K A, Hanan E J, et al. RTK-dependent inducible degradation of mutant PI3Kα drives GDC-0077 (Inavolisib) efficacy[J]. Cancer discovery, 2022, 12(1): 204-219.

Product Documents

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
2060571-02-8
Synonyms
GDC-0077; RG6114
SMILES
C[C@@H](C(N)=O)NC1=CC=C(C2=NC(N3[C@H](C(F)F)COC3=O)=CN2CCO4)C4=C1
Molecular Formula
C18H19F2N5O4
Molecular Weight
407.37
Solubility
DMSO : ≥ 180 mg/mL (441.86 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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