[CAS NO. 1404456-53-6] GSK2830371

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PRODUCTS SPECIFICATIONS [1404456-53-6]

Catalog

HY-15832

Brand

MCE

CAS

1404456-53-6

DESCRIPTION [1404456-53-6]

Overview

MDL	MFCD28009442
Molecular Weight	461.02
Molecular Formula	C23H29ClN4O2S
SMILES	ClC1=CN=C(C)C(NCC2=CC=C(C(N[C@@H](CC3CCCC3)C(NC4CC4)=O)=O)S2)=C1

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

10 Publications Citing Use of MCE

Summary

GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC ₅₀ of 6 nM.

IC50 & Target

IC50: 6 nM (Wip1 phosphatase) ^[1]

In Vitro

GSK 2830371 potently inhibits Wip1 (2-420) dephosphorylation of FDP and the endogenous substrates phospho-p38 MAPK (T180) with IC ₅₀ values of 6 nM and 13 nM, respectively. In the PPM1D -amplified MCF7 breast carcinoma cells, treatment with GSK 2830371 (0.04, 0.11, 0.33, 1, 3, and 9 μM) increased phosphorylation of substrates in a concentration-dependent manner. Treatment of MX-1 and MCF7 cells (Wip1amplified, p53 wild type) with GSK 2830371 (0.001, 0.01, 0.1, 1, and 10 μM) causes concentration-dependent effects in cell growth assays ^[1] . GSK2830371 has a 50% growth inhibitory concentration (GI ₅₀ ) of 2.65 μM±0.54 (SEM) in MCF-7 cells. Treatment of MCF-7 cells with 2.5μM GSK2830371 results in marked time-dependent degradation of both isoforms of WIP1 over 8 hours which correlated with p53 stabilisation and phospho-p53 ^Ser15 (pp53 ^Ser15 ) ^[2] .

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

In Vivo

In a pharmacodynamic assay, orally administered GSK 2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreased Wip1protein concentrations in DOHH2 tumors. Following 14 d of oral dosing at 150 mg per kg body weight, BID (twice daily) and TID (thrice daily), GSK 2830371 inhibits the growth of DOHH2 tumor xenografts by 41% and 68%, respectively. Comparable tumor growth inhibition is observed in mice treated BID with either 75 or 150 mg per kg body weight. Greater tumor growth inhibition with the TID schedule is consistent with a short half-life of GSK 2830371 in mice and suggests that sustained inhibition of Wip1 may be required for maximal antitumor effect ^[1] .

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 : ≥ 51 mg/mL ( 110.62 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1691 mL	10.8455 mL	21.6910 mL
5 mM	0.4338 mL	2.1691 mL	4.3382 mL
10 mM	0.2169 mL	1.0846 mL	2.1691 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 (5.42 mM); Clear solution
2.

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

Solubility: 2.5 mg/mL (5.42 mM); Suspended solution; Need ultrasonic
3.

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

Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

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