[CAS NO. 1619983-52-6] AQX-435

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PRODUCTS SPECIFICATIONS [1619983-52-6]

Catalog

HY-136268

Brand

MCE

CAS

1619983-52-6

DESCRIPTION [1619983-52-6]

Overview

MDL	-
Molecular Weight	450.57
Molecular Formula	C27H34N2O4
SMILES	O=C(C1=CC=CN=C1)N[C@@H]2C[C@@]3([H])C(C)(C)CCC[C@]3(C)[C@@H](C(C4=CC(O)=CC(O)=C4)=O)[C@@H]2C

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

Summary

AQX-435 is a potent SHIP1 phosphatase activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth ^[1] ^[2] .

In Vitro

AQX-435 reduces CLL cell viability in a dose-dependent manner ^[1] .
AQX-435-induced (5-30 µM; 24 hours) apoptosis is mediated via caspases since AQX435 induced PARP cleavage ^[1] .
AQX-435 effectively inhibits PI(3,4,5)P3-mediated signaling downstream of the BCR in CLL and DLBCL cells ^[1] . AQX-435 and Ibrutinib combine effectively to enhanced inhibition of BCR signaling. AQX-435 induced TMD8 cell apoptosis in vitro with an IC ₅₀ of ~2 µM. AQX-435 reduces anti-IgM-induced AKT phosphorylation and induces apoptosis in DLBCL cells ^[1] .

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

Cell Viability Assay ^[1]

Cell Line:	Chronic lymphocytic leukemia (CLL) cells
Concentration:	5-30 µM
Incubation Time:	24 hours
Result:	Reduced CLL cell viability in a dose-dependent manner.

In Vivo

AQX-435 (10 mg/kg; i.p.; 5 days) significantly reduced the volume of TMD8 tumors ^[1] .
AQX-435 (50 mg/kg; ip) inhibits DLBCL PDX tumors growth ^[1] .
AQX-435 reduced AKT phosphorylation and growth of DLBCL in vivo and cooperated with ibrutinib for tumor growth inhibition ^[1] .

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

Animal Model:	NOD.Cg-Prkdc scidIl2rgtm1Wjl/SzJ mice (NSG mice) (TMD8 tumors) ^[1]
Dosage:	10 mg/kg
Administration:	I.p.; in 7-day cycles each comprising 5 days of AQX-435 followed by 2 days with no drug
Result:	Reduced the volume of TMD8 tumors.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 221.94 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2194 mL	11.0971 mL	22.1941 mL
5 mM	0.4439 mL	2.2194 mL	4.4388 mL
10 mM	0.2219 mL	1.1097 mL	2.2194 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 (5.55 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.55 mM); Clear solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% Corn Oil

Solubility: 2.5 mg/mL (5.55 mM); Clear solution; Need ultrasonic

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