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[CAS NO. 502632-66-8] Sonolisib
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-N6775 |
| Brand: | MCE |
| CAS: | 502632-66-8 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 525.59 |
| Molecular Formula | C29H35NO8 |
| SMILES | O=C1C([C@@](CC2)([H])[C@@]3(C)C2=O)=C([C@H](OC(C)=O)C3)[C@]4(C)C(/C(C(O[C@@H]4COC)=O)=C\N(CC=C)CC=C)=C1O |
1 Publications Citing Use of MCE
Summary
IC50 & Target
|
p110α 0.1 nM (IC 50 ) |
p110δ 2.9 nM (IC 50 ) |
p120γ 1 nM (IC 50 ) |
In Vitro
Sonolisib (PX-866) 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 [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01259869 | NCIC Clinical Trials Group|Cascadian Therapeutics Inc.|Canadian Cancer Trials Group |
Glioblastoma
|
December 9, 2010 | Phase 2 |
| NCT01252628 | Cascadian Therapeutics Inc.|Seagen Inc. |
Incurable Metastatic Colorectal Carcinoma|Incurable Progressive, Recurrent or Metastatic Squamous Cell Carcinoma of the Head and Neck
|
December 2010 | Phase 1|Phase 2 |
| NCT01331083 | NCIC Clinical Trials Group|Oncothyreon Canada Inc.|Canadian Cancer Trials Group |
Prostate Cancer
|
April 4, 2011 | Phase 2 |
| NCT01616199 | Cascadian Therapeutics Inc.|Seagen Inc. |
Advanced BRAF-mutant Cancers
|
August 2012 | Phase 1|Phase 2 |
| NCT01408316 | Cascadian Therapeutics Inc.|Seagen Inc. |
Healthy Volunteer
|
July 2011 | Phase 1 |
| NCT00726583 | Cascadian Therapeutics Inc.|Seagen Inc. |
Advanced Solid Tumors
|
June 2008 | Phase 1 |
| NCT01204099 | Cascadian Therapeutics Inc.|Seagen Inc. |
Non Small Cell Lung Cancer (NSCLC)|Squamous Cell Carcinoma of the Head and Neck (SCCHN)
|
September 2010 | Phase 1|Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 190.26 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
References
- [1] Ihle NT, et al. The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growthfactor receptor inhibitor ZD1839 in A-549 human non-small cell lung cancer xenografts. Mol Cancer Ther. 2005 Sep;4(9):1349-57.
- [2] Bowles DW, et al. A Randomized, Phase II Trial of C225 With or Without PX-866, an Irreversible Oral Phosphatidylinositol 3-Kinase Inhibitor, in Patients With Metastatic Colorectal Carcinoma. Clin Colorectal Cancer. 2016 Dec;15(4):337-344.e2.
- [3] Sonolisib
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