PRT543 | PRMT5 inhibitor | Probechem Biochemicals

Chemical Structure : PRT543

CAS No.: 1989620-03-2

PRT543 (PRT-543, PRT 543)

Catalog No.: PC-21272Not For Human Use, Lab Use Only.

PRT543 is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 10.8 nM.

Packing	Price	Stock
5 mg	$128	In stock
10 mg	$198	In stock
25 mg	$348	In stock
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Biological Activity

PRT543 is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 10.8 nM.

PRT543 induced significant dose-related tumor growth inhibition at well-tolerated doses in cell-line derived xenograft (CDX) models harboring the U2AF1S34F or RBM10LOF mutation.

PRT543 decreased expression of DNA damage repair-associated genes (e.g. BRCA1, RAD51AP1, FANCA, and FANCL) in U2AF1S34F or RBM10LOF mutant NSCLC cells.

Combination with PRT543 increased the effectiveness of specific chemotherapeutic agents in both in vitro and in vivo (CDX) models of U2AF1S34F and RBM10LOF NSCLC.

Physicochemical Properties

M.Wt	376.80
Formula	C17H17ClN4O4
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(2R,3R,4S,5R)-2-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-((R)-(4-chlorophenyl)(hydroxy)methyl)tetrahydrofuran-3,4-diol

References

1. Carter J, et al. Cancer Res Commun. 2023 Nov 6;3(11):2233-2243.
2. Jack Carter, et al. Cancer Res (2022) 82 (12_Supplement): 2159.

PRT543 (PRT-543, PRT 543)

Biological Activity

Physicochemical Properties

References

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