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GDC-0326 

Cat. No.: HY-101272 Purity: 99.31%
Handling Instructions

GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.

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

GDC-0326 Chemical Structure

GDC-0326 Chemical Structure

CAS No. : 1282514-88-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 192 In-stock
Estimated Time of Arrival: December 31
25 mg USD 444 In-stock
Estimated Time of Arrival: December 31
50 mg USD 804 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.

IC50 & Target[1]

PI3Kα

0.2 nM (Ki)

PI3Kδ

4 nM (Ki)

PI3Kγ

10.2 nM (Ki)

PI3Kβ

26.6 nM (Ki)

In Vitro

GDC-0326 is highly selective over other kinases. In a panel of 235 kinases, only one is inhibited by >50% by GDC-0326 when tested at 1 µM. GDC-0326 is not an inhibitor of cytochrome P450 enzymes tested (IC50>10 µM against 3A4, 2C9 1A2, 2C19, 2D6), is highly permeable in MDCK cells and has thermodynamic solubility of 82 µg/mL at pH 7.4[1].

In Vivo

GDC-0326 is highly stable in human and rat liver microsomes, and there is a good correlation with in vivo rat clearance. It is found to have consistently low clearance and high oral bioavailability across species tested, enabling significant sustained free drug levels. Daily administration of GDC-0326 orally at 0.78, 1.56, 3.25, 6.25, or 12.5 mg/kg results in dose-dependent increase in TGI (73%, 79%, 83%, 101%, and 110%, respectively) and tumor regressions (6 PRs out of 10 animal at 6.25 and 12.5 mg/kg) when compared to vehicle treated mice. Daily administration of GDC-0326 orally at 0.78, 1.56, 3.25, 6.25, or 12.5 mg/kg also results in dose-dependent increase in TGI (73%, 97%, 97%, 122%, and 121%, respectively) in the KPL-4 xenograft model. Notably, maximum efficacy of GDC-0326 is observed at 6.25 mg/kg in the KPL-4 model based on TGI and tumor regressions (9 PRs and 1 CR out of 10 animal treated) when compared to vehicle treated mice. Doses of GDC-0326 up to 12.5 mg/kg are well tolerated based on less than 10% body weight loss (data not shown)[1].

Molecular Weight

382.42

Formula

C₁₉H₂₂N₆O₃

CAS No.

1282514-88-8

SMILES

C[[email protected]](OC1=CC=C2C3=NC(C4=NC=NN4C(C)C)=CN3CCOC2=C1)C(N)=O

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 : ≥ 83.3 mg/mL (217.82 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6149 mL 13.0746 mL 26.1493 mL
5 mM 0.5230 mL 2.6149 mL 5.2299 mL
10 mM 0.2615 mL 1.3075 mL 2.6149 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats: Male Sprague-Dawley rats are dosed intravenously with 1 mg/kg of GDC-0326 prepared in 60% PEG400/10% Ethanol. Male Sprague-Dawley rats are dosed PO with 5 mg/kg of GDC-0326 in 0.5% methylcellulose with 0.2% Tween 80 (MCT)[1].

Mice: Female NCR nude mice are dosed intravenously with 1 mg/kg of GDC-0326 prepared in 60% PEG400/10% Ethanol and PO at 25 mg/kg in 0.5% methylcellulose with 0.2% Tween 80 (MCT)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

GDC-0326GDC0326GDC 0326PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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GDC-0326
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