[CAS NO. 2109805-87-8] FEN1-IN-3

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PRODUCTS SPECIFICATIONS [2109805-87-8]

Catalog

HY-136484

Brand

MCE

CAS

2109805-87-8

DESCRIPTION [2109805-87-8]

Overview

MDL	-
Molecular Weight	284.27
Molecular Formula	C15H12N2O4
SMILES	O=C(N1O)N(C2=CC=C(OC)C=C2)C3=C(C=CC=C3)C1=O

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

Summary

FEN1-IN-3 (Compound 4) is a human flap endonuclease-1 ( hFEN1 ) inhibitor. FEN1-IN-3 stabilizes hFEN1 with an EC ₅₀ of 6.8 μM ^[1] .

In Vitro

FEN1 inhibition selectively impairs proliferation of colon cancer cells deficient in Cdc4 and Mre11a , both frequently mutated in colorectal cancers. FEN1 has also emerged as a potential chemosensitizing target due to its role in LP-BER since it is critical for repair of Methyl methanesulfonate-induced alkylation damage, and its knockdown or inhibition increases sensitivity to Temozolomide in glioblastoma and colorectal cancer cell lines ^[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 : 250 mg/mL ( 879.45 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5178 mL	17.5889 mL	35.1778 mL
5 mM	0.7036 mL	3.5178 mL	7.0356 mL
10 mM	0.3518 mL	1.7589 mL	3.5178 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 (7.32 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (7.32 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (7.32 mM); Clear solution

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

References

[1] Jack C Exell, et al. Cellularly Active N-hydroxyurea FEN1 Inhibitors Block Substrate Entry to the Active Site. Nat Chem Biol. 2016 Oct;12(10):815-21.