| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
With a Ki of 0.2 nM, GDC-0326 is a brand-new, powerful, and selective PI3K (-Isoform of Phosphoinositide 3-Kinase) inhibitor. Inhibitors of the class I phosphoinositide 3-kinase (PI3K) isoform PI3Kα have drawn a lot of interest due to their potential application in the treatment of cancer. Despite the particular appeal of targeting PI3Kα , it has proven difficult to inhibit this isoform with selectivity. High selectivity is demonstrated by GDC-0326 versus other kinases. In humans, GDC-0326 has a low plasma CL. There are four class I PI3K isoforms (α, β, δ, and γ) ) in the PI3 kinase family. PI3K is the isoform of these that is most frequently linked to cancer.
| Targets |
PI3Kα (Ki = 0.2 nM); PI3Kβ (Ki = 26.6 nM); PI3Kδ (Ki = 4 nM); PI3Kγ (Ki = 10.2 nM)
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| ln Vitro |
The PI3Kα specific inhibitor GDC-0326 also achieves a very high level of selectivity over other kinases in addition to selectivity over the other class I isoforms. When tested on cytochrome P450 enzymes, GDC-0326 was not an inhibitor[1].
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| ln Vivo |
GDC-0326 has a consistently low clearance and a high oral bioavailability in all tested species, allowing for significant sustained free drug levels[1].
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| Cell Assay |
At 1 × 106 cells per dish, TC3 cells are plated. Cells are treated for 2 hours with vehicle, GDC-0941 (1 μM), GDC-0326 (1 μM), TGX-221 (0.5 μM), IC87114 (5 μM), BKM120 (0.8 μM) or BYL719 (1 μM) 24 hours later, after which they are lysed.
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| Animal Protocol |
Mice: GDC-0326 is administered intravenously to female NCR nude mice at a dose of 1 mg/kg in a solution of 60% PEG400/ 10% ethanol and orally at a dose of 25 mg/kg in a solution of 0.5% methylcellulose/ 0.2% Tween 80 (MCT). Rats: 1 mg/kg of GDC-0326 prepared in 60% PEG400/10% ethanol is administered intravenously to male Sprague-Dawley rats. Male Sprague-Dawley rats are administered 5 mg/kg of GDC-0326 orally (PO) in a 0.5% methylcellulose/0.2% Tween 80 (MCT) solution.
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| References |
| Molecular Formula |
C19H22N6O3
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|---|---|
| Molecular Weight |
382.416383266449
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| Exact Mass |
382.1753
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| Elemental Analysis |
C, 59.67; H, 5.80; N, 21.98; O, 12.55
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| CAS # |
1282514-88-8
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| Related CAS # |
1282514-88-8
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| Appearance |
Solid powder
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| SMILES |
C[C@@H](C(=O)N)OC1=CC2=C(C=C1)C3=NC(=CN3CCO2)C4=NC=NN4C(C)C
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| InChi Key |
SIKYDKLGPWRPMZ-LBPRGKRZSA-N
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| InChi Code |
InChI=1S/C19H22N6O3/c1-11(2)25-19(21-10-22-25)15-9-24-6-7-27-16-8-13(28-12(3)17(20)26)4-5-14(16)18(24)23-15/h4-5,8-12H,6-7H2,1-3H3,(H2,20,26)/t12-/m0/s1
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| Chemical Name |
(2S)-2-[[2-(2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]oxy]propanamide
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| Synonyms |
GDC-0326; GDC 0326; GDC0326
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 76~100 mg/mL (198.7~261.5mM)
Ethanol: ~19 mg/mL (~49.7 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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