[CAS NO. 502632-66-8] Sonolisib

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PRODUCTS SPECIFICATIONS [502632-66-8]

Catalog

HY-N6775

Brand

MCE

CAS

502632-66-8

DESCRIPTION [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

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

1 Publications Citing Use of MCE

[1]Research Square Preprint. 2022 Jul.

Summary

Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K ( IC ₅₀ =0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity ^[1] ^[2] .

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

In Vitro:

DMSO : 100 mg/mL ( 190.26 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
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

* All of the co-solvents are available by MCE.