GDC-0326

Name: GDC-0326
Brand: MedChemExpress
SKU: HY-101272
Rating: 5.0 (1 reviews)

Cat. No.: HY-101272 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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

GDC-0326 Chemical Structure

CAS No. : 1282514-88-8

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 118	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 118	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 40	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 325	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

GDC-0326 is a potent and selective PI3Kα inhibitor with a K_i 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].

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

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].

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

Molecular Weight

382.42

Formula

C₁₉H₂₂N₆O₃

CAS No.

1282514-88-8

Appearance

Solid

Color

White to off-white

SMILES

C[C@H](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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (261.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (250 KB) SDS (0 KB)

COA (252 KB) HNMR (142 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Heffron TP, et al. The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326). J Med Chem. 2016 Feb 11;59(3):985-1002. [Content Brief]

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

[1]. Heffron TP, et al. The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326). J Med Chem. 2016 Feb 11;59(3):985-1002. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6149 mL	13.0746 mL	26.1493 mL	65.3731 mL
	5 mM	0.5230 mL	2.6149 mL	5.2299 mL	13.0746 mL
	10 mM	0.2615 mL	1.3075 mL	2.6149 mL	6.5373 mL
	15 mM	0.1743 mL	0.8716 mL	1.7433 mL	4.3582 mL
	20 mM	0.1307 mL	0.6537 mL	1.3075 mL	3.2687 mL
	25 mM	0.1046 mL	0.5230 mL	1.0460 mL	2.6149 mL
	30 mM	0.0872 mL	0.4358 mL	0.8716 mL	2.1791 mL
	40 mM	0.0654 mL	0.3269 mL	0.6537 mL	1.6343 mL
	50 mM	0.0523 mL	0.2615 mL	0.5230 mL	1.3075 mL
	60 mM	0.0436 mL	0.2179 mL	0.4358 mL	1.0896 mL
	80 mM	0.0327 mL	0.1634 mL	0.3269 mL	0.8172 mL
	100 mM	0.0261 mL	0.1307 mL	0.2615 mL	0.6537 mL

GDC-0326 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GDC-03261282514-88-8GDC0326GDC 0326PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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GDC-0326

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Biological Activity

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GDC-0326 Related Antibodies

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Complete Stock Solution Preparation Table

GDC-0326 Related Classifications

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