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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Sonolisib (also known as PX-866)is a novel, oral, irreversible, and pan-isoform small-molecule inhibitor of phosphoinositide 3-kinase/PI3K with potential anticancer activity (IC50=0.1 nM (p110α), 1.0 nM (p120γ), and 2.9 nM (p110δ). anti-tumor effects. Sonolisib prevents the secondary messenger phosphatidylinositol-3,4,5-triphosphate (PIP3) from being produced and the PI3K/Akt signaling pathway from being activated, which may prevent the growth and survival of tumor cells in populations of tumor cells that are susceptible to this effect. The PI3K/Akt signaling pathway is frequently involved in the development of tumors, and aberrant PI3K/Akt signaling may play a role in the development of tumor resistance to a range of antineoplastic agents.
| Targets |
p110α (IC50 = 0.1 nM); p110δ (IC50 = 2.9 nM); p120γ (IC50 = 1 nM)
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|---|---|
| ln Vitro |
Sonolisib (PX-866) suppresses the activation of PI3K/Akt signaling and the phospholipid messenger phosphoinositol-3,4,5-trisphosphate (PIP3), which may suppress the proliferation of tumor cells and vulnerable tumor cell populations [3].
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| References |
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| Additional Infomation |
PX-866 is an organic heterotetracyclic compound that is obtained from wortmanin via aminolysis of its furan ring by diallyl amine. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor. It is an organic heterotetracyclic compound, a delta-lactone, an acetate ester and a tertiary amino compound. It is functionally related to a wortmannin.
Sonolisib has been used in trials studying the treatment of Glioblastoma, Prostate Cancer, Advanced Solid Tumors, Advanced BRAF-mutant Cancers, and Non Small Cell Lung Cancer (NSCLC), among others. Sonolisib is a small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. Sonolisib inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. |
| Molecular Formula |
C29H35NO8
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|---|---|
| Molecular Weight |
525.5901
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| Exact Mass |
525.236
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| Elemental Analysis |
C, 66.27; H, 6.71; N, 2.66; O, 24.35
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| CAS # |
502632-66-8
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| Related CAS # |
502632-66-8
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| PubChem CID |
9849735
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| Appearance |
Yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
651.4±55.0 °C at 760 mmHg
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| Flash Point |
347.7±31.5 °C
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| Vapour Pressure |
0.0±4.4 mmHg at 25°C
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| Index of Refraction |
1.586
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| LogP |
2.37
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
38
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| Complexity |
1200
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C=CCN(CC=C)/C=C\1/C2=C(C(=O)C3=C(C(CC4(C)C3CCC4=O)OC(=O)C)C2(C)C(COC)OC1=O)O
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| InChi Key |
QIUASFSNWYMDFS-NILGECQDSA-N
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| InChi Code |
InChI=1S/C29H35NO8/c1-7-11-30(12-8-2)14-17-23-26(34)25(33)22-18-9-10-20(32)28(18,4)13-19(37-16(3)31)24(22)29(23,5)21(15-36-6)38-27(17)35/h7-8,14,18-19,21,34H,1-2,9-13,15H2,3-6H3/b17-14+/t18-,19+,21+,28-,29-/m0/s1
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| Chemical Name |
(4S,4aR,5R,6aS,9aR,E)-1-((diallylamino)methylene)-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,7,10-trioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate
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| Synonyms |
Sonolisib; PX 866; PX866; PX866
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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: ~100 mg/mL (190.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.76 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 (4.76 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9026 mL | 9.5131 mL | 19.0262 mL | |
| 5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL | |
| 10 mM | 0.1903 mL | 0.9513 mL | 1.9026 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.
| NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01408316 | Completed | Drug: PX-866 | Healthy Volunteer | Cascadian Therapeutics Inc. | July 2011 | Phase 1 |
| NCT00726583 | Completed | Drug: PX-866 | Advanced Solid Tumors | Cascadian Therapeutics Inc. | June 2008 | Phase 1 |
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