[CAS NO. 1637770-13-8] GS-626510

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PRODUCTS SPECIFICATIONS [1637770-13-8]

Catalog

AS967858

Brand

Arctom Scientific

CAS

1637770-13-8

DESCRIPTION [1637770-13-8]

Overview

MDL	-
Molecular Weight	394.47
Molecular Formula	C25H22N4O
SMILES	CC1=C(C2=CC(C3=C4C=CC=NC4=CC=C3C)=C5NC(C6CC6)=NC5=C2)C(C)=NO1

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

Summary

GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with K _d values of 0.59-3.2 nM for BRD2/3/4, with IC ₅₀ values of 83 nM and 78 nM foe BD1 and BD2 , respectively ^[1] .

IC50 & Target

BRD2

0.59-2.5 nM (Kd)

BRD3

0.65-0.66 nM (Kd)

BRD4

1.3-3.2 nM (Kd)

BD1

83 nM (IC ₅₀ )

BD2

78 nM (IC ₅₀ )

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 : 25 mg/mL ( 63.38 mM ; ultrasonic and warming and adjust pH to 4 with HCl and heat to 80°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5350 mL	12.6752 mL	25.3505 mL
5 mM	0.5070 mL	2.5350 mL	5.0701 mL
10 mM	0.2535 mL	1.2675 mL	2.5350 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 (6.34 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

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

References

[1] Sperandio D, et al. Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor. Bioorg Med Chem. 2019 Feb 1;27(3):457-469.