1. PI3K/Akt/mTOR
    Apoptosis
  2. PI3K
    Apoptosis
  3. GDC-0077

GDC-0077 (Synonyms: RG6114)

Cat. No.: HY-101562 Purity: 98.94%
Handling Instructions

GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.

For research use only. We do not sell to patients.

GDC-0077 Chemical Structure

GDC-0077 Chemical Structure

CAS No. : 2060571-02-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 594 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 900 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1260 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2020 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3280 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα[1].

IC50 & Target[1]

PI3Kα

0.038 nM (IC50)

In Vitro

GDC-0077 (RG6114) 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 selectively degrades mutant PI3Kα in a proteasome-dependent fashion resulting in reduction of PI3K pathway activity biomarkers such as pAKT and pPRAS40, inhibition of cell proliferation, and increased apoptosis in human PIK3CA-mutant breast cancer cell lines to a greater extent when compared to PIK3CA wild-type cells[1].

In Vivo

GDC-0077 (p.o.) results in tumor regressions, induction of apoptosis, and a reduction of pAKT, pPRAS40, and pS6RP in a dose-dependent fashion in patient-derived PIK3CA-mutant breast cancer xenograft models[1].

Clinical Trial
Molecular Weight

407.37

Formula

C₁₈H₁₉F₂N₅O₄

CAS No.

2060571-02-8

SMILES

C[[email protected]@H](C(N)=O)NC1=CC=C(C2=NC(N3[[email protected]](C(F)F)COC3=O)=CN2CCO4)C4=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 180 mg/mL (441.86 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4548 mL 12.2739 mL 24.5477 mL
5 mM 0.4910 mL 2.4548 mL 4.9095 mL
10 mM 0.2455 mL 1.2274 mL 2.4548 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 98.94%

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Keywords:

GDC-0077RG6114GDC0077GDC 0077RG 6114RG-6114PI3KApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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GDC-0077
Cat. No.:
HY-101562
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