[CAS NO. 1941211-99-9] LSN 3213128

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PRODUCTS SPECIFICATIONS [1941211-99-9]

Catalog

HY-107981

Brand

MCE

CAS

1941211-99-9

DESCRIPTION [1941211-99-9]

Overview

MDL	-
Molecular Weight	409.46
Molecular Formula	C17H16FN3O4S2
SMILES	O=C1NC=CC2=C1C=C(NS(=O)(C3=CC=C(N4CC[C@@H](O)C4)S3)=O)C(F)=C2

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

Summary

LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase ( AICARFT ), with IC ₅₀ of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity ^[1] .

IC50 & Target

IC50: 16 nM (AICARFT), 19 nM (AICARFT in cells) ^[1]

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 : 62.5 mg/mL ( 152.64 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4422 mL	12.2112 mL	24.4224 mL
5 mM	0.4884 mL	2.4422 mL	4.8845 mL
10 mM	0.2442 mL	1.2211 mL	2.4422 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 (5.08 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

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

References

[1] Fales KR, et al. Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransfera