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ART812

Catalog No. T40236 CAS 2607138-82-7

ART812 is an orally active inhibitor of DNA polymerase Polθ, possessing an IC50 value of 7.6 nM. Additionally, ART812 exhibits a cell-based microhomology-mediated end joining (MMEJ) IC50 value of 240 nM.

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ART812, CAS 2607138-82-7

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	ART812 is an orally active inhibitor of DNA polymerase Polθ, possessing an IC50 value of 7.6 nM. Additionally, ART812 exhibits a cell-based microhomology-mediated end joining (MMEJ) IC50 value of 240 nM.
Targets&IC50	Polθ:7.6 nM (IC50)
In vitro	ART812 (0-40 μM) elicits Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells [1] .
In vivo	ART812 (100?mg/kg; p.o. daily for 76 days) shows significant tumour inhibition in rats bearing established MDA-MB-436 BRCA1/SHLD2 defective tumours (volume 250-350?mm 3 ) [1] .

Molecular Weight	461.8
Formula	C19H16ClF4N3O4
CAS No.	2607138-82-7

Storage

store at low temperature

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 90.0 mg/mL (194.9 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Zatreanu D, et al. Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance. Nat Commun. 2021 Jun 17;12(1):3636. 2. Peter BLENCOWE, et al. Preparation of heterocyclic compounds for use in the treatment of cancer. WO2021028643 A1.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

ART812 2607138-82-7 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis ART-812 Inhibitor inhibitor inhibit

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