[CAS NO. 2244452-09-1] BI-4924

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PRODUCTS SPECIFICATIONS [2244452-09-1]

Catalog

HY-126254

Brand

MCE

CAS

2244452-09-1

DESCRIPTION [2244452-09-1]

Overview

MDL	-
Molecular Weight	499.36
Molecular Formula	C21H20Cl2N2O6S
SMILES	O=C(O)CS(=O)(C1=CC=C([C@H](NC(C(N2C)=CC3=C2C=C(C)C(Cl)=C3Cl)=O)CO)C=C1)=O

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

1 Publications Citing Use of MCE

[1]Nat Commun. 2022 May 16;13(1):2698.

Summary

BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase ( PHGDH ) inhibitor ( IC ₅₀ =3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC ₅₀ of 2200 nM at 72 h ^[1] .

IC50 & Target

PHGDH ^[1]

In Vitro

BI-4924 is a highly potent co-factor nicotinamide adenine dinucleotide (NADH/NAD ⁺ )-competitive PHGDH inhibitor. BI-4924 shows high selectivity against the majority of other dehydrogenase targets ^[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 : 125 mg/mL ( 250.32 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0026 mL	10.0128 mL	20.0256 mL
5 mM	0.4005 mL	2.0026 mL	4.0051 mL
10 mM	0.2003 mL	1.0013 mL	2.0026 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: ≥ 2.08 mg/mL (4.17 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution

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

References

[1] Weinstabl H, et al. Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis. J Med Chem. 2019 Jul 31.