[CAS NO. 284028-89-3] XAV-939

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PRODUCTS SPECIFICATIONS [284028-89-3]

Catalog

HY-15147

Brand

MCE

CAS

284028-89-3

DESCRIPTION [284028-89-3]

Overview

MDL	MFCD16879017
Molecular Weight	312.31
Molecular Formula	C14H11F3N2OS
SMILES	O=C1C(CSCC2)=C2N=C(C3=CC=C(C(F)(F)F)C=C3)N1

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

86 Publications Citing Use of MCE

Summary

XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC ₅₀ values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer , fibrotic diseases and conditions associated with low bone formation ^[1] ^[2] ^[3] .

IC50 & Target

TNKS2

2 nM (IC ₅₀ )

TNKS1

5 nM (IC ₅₀ )

ARTD2

479 nM (IC ₅₀ )

ARTD1

5500 nM (IC ₅₀ )

In Vitro

XAV-939 has activity against TNKS1 and TNKS2 with IC ₅₀ values of 5 nM and 2 nM, respectively ^[1] .
XAV-939 (0.3-30 μM; 3 or 10 days) enhances osteoblast differentiation of hBMSCs ^[2] .
XAV-939 (3 μM) promotes osteoblast differentiation of hMSCs via accumulation of SH3BP2 ^[2] .
XAV-939 (3 μM; 10 days) upregulates the expression of OPG and downregulates the expression of RANKL in hBMSCs during osteoblast differentiation ^[2] .
XAV-939 suppresses Wnt/β-catenin signaling and promotes SFRP3 and SFRP4 expression ^[3] .

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

Cell Viability Assay ^[2]

Cell Line:	hMSC-TERT cell line
Concentration:	0.3, 3, and 30 μM
Incubation Time:	3 days
Result:	Showed no significant effect on proliferation at day 1, 2, and 3 at dose of 0.3 and 3 μM but inhibited hMSCs cell proliferation on day 3 at dose of 30 μM.

Apoptosis Analysis ^[2]

Cell Line:	hMSC-TERT cell line
Concentration:	3 µM
Incubation Time:	3 days
Result:	Showed a minute percentage of cell death (apoptosis and necrosis) in the XAV-939-treated hBMSC

RT-PCR ^[2]

Cell Line:	hMSC-TERT cell line
Concentration:	3 µM
Incubation Time:	10 days
Result:	Upregulated gene expression of osteoblast-associated gene markers including: ALP, COL1A1, RUNX2, and OC.

In Vivo

XAV-939 rescues mechanical stress-induced cartilage degeneration in vivo ^[3] .

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

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 : 15.62 mg/mL ( 50.01 mM ; ultrasonic and warming and heat to 60°C)

H ₂ O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2019 mL	16.0097 mL	32.0195 mL
5 mM	0.6404 mL	3.2019 mL	6.4039 mL
10 mM	0.3202 mL	1.6010 mL	3.2019 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: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic
2.

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

Solubility: 1.56 mg/mL (5.00 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: 1.56 mg/mL (5.00 mM); Clear solution; Need ultrasonic

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