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Cat. No.: HY-123599

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IACS-4619

IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC₅₀=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target.

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

CAS No.: 1884209-98-6
Formula: C₁₀H₁₇N₃O
Molecular Weight:195.27

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (279 KB)

IACS-4619 Chemical Structure

CAS No.: 1884209-98-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
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- In Vitro
Chemical Information
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Biological Activity

Description

All DNA/RNA Synthesis Isoforms :

In Vitro

IACS-4619 shows good MDCK cell permeability, high human plasma protein binding, high liver microsomal turnover, and good plasma stability in rats and humans^[1].
IACS-4619 (up to 50 μM) does not confer a robust anti-proliferative phenotype in human cancer cell lines (U2OS, SaOS2, etc.) and normal cell lines (WI38, BJ, etc.)^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

Human cancer cell lines (U2OS, SaOS2, SW480, HCT116, MDAMB231, HeLa, UOK262, 293T, A549, H460, H358) and normal cell lines (WI38, BJ, hMEC, MRC5)
Concentration:

0-50 μM
Incubation Time:

/
Result:

Did not exhibit significant antiproliferative effects or cytotoxicity in any tested cell lines, even with prolonged treatment, and cell lines with high intrinsic ROS levels tolerated the compound well.

Chemical Information

CAS No. 1884209-98-6
Molecular Weight 195.27
Formula C₁₀H₁₇N₃O
SMILES

N=1C=C(C(=NC1N)OCC(C)(C)C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Petrocchi A, et al. Identification of potent and selective MTH1 inhibitors. Bioorg Med Chem Lett. 2016;26(6):1503-1507. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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References

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IACS-4619

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

IACS-4619 Related Classifications

HY-123599 Related Classifications