ART812 free base · Synonyms: ART-812 · ART 812

ART812 is an orally active DNA polymerase Polθ inhibitor.

For research use only. Not for human or veterinary use.

Target DNA/RNA Synthesis

Research area Cancer

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Data Sheet SDS COA

ART812 structure

CAS No.: 2607138-82-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 450.00	BP-02035-25mg	In stock	Get quote
50 mg	USD 670.00	BP-02035-50mg	In stock	Get quote
100 mg	USD 972.00	BP-02035-100mg	In stock	Get quote
250 mg	USD 1,450.00	BP-02035-250mg	In stock	Get quote
500 mg	USD 2,050.00	BP-02035-500mg	In stock	Get quote
1 g	USD 2,850.00	BP-02035-1g	In stock	Get quote

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Description

ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 has an IC50 value of 240 nM for cell based microhomology-mediated end joining (MMEJ).

Biological activity

ART812 (0-40 μM) elicits Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells 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 mm3)

Identifiers

SMILES: CN(C1=CC(Cl)=C(C=C1)F)C([C@H]2N(C3=CC(C(F)(F)F)=CC(C)=N3)C([C@H]([C@H]2O)O)=O)=O
InChIKey: YJJOABOMFPGRED-JYJNAYRXSA-N

Specifications

MW (average): 461.7950
Formula: C₁₉H₁₆ClF₄N₃O₄
CAS No.: 2607138-82-7
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

[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.

Same target

Search DNA/RNA Synthesis

Same research area

Search Cancer