CRCD2 | NT5C2 inhibitor | Probechem Biochemicals

Chemical Structure : CRCD2

CAS No.: 941185-83-7

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CRCD2 (NT5C2 inhibitor)

货号: PC-49276Not For Human Use, Lab Use Only.

CRCD2 is a first-in-class specific small molecule inhibitor of the cytosolic 5' nucleotidase II (NT5C2), directly binds to NT5C2 R367Q recombinant protein with KD of 70.9 uM, shows broadly activies against leukemias bearing highly prevalent relapse-associated mutant forms of NT5C2 in vitro and in vivo.

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生物&药学活性

CRCD2 is a first-in-class specific small molecule inhibitor of the cytosolic 5' nucleotidase II (NT5C2), directly binds to NT5C2 R367Q recombinant protein with KD of 70.9 uM, shows broadly activies against leukemias bearing highly prevalent relapse-associated mutant forms of NT5C2 in vitro and in vivo.
CRCD2 displays dose-dependent low micromolar inhibitory capacity against both NT5C2 wild-type and the R367Q mutant and significantly reduces NT5C2 K359Q nucleotidase activity.
CRCD2 treatment enhances the cytotoxic activity of 6-MP in NT5C2 wild type leukemias.
CRCD2 reverses genetic and non-genetic drivers of 6-MP resistance in acute lymphoblastic leukemia.
NT5C2 inhibitor CRCD2 sensitizes both NT5C2 WT (Nt5c2+/co-R367Q) and NT5C2 mutant (Nt5c2+/R367Q) mouse lymphoblasts to 6-MP.

物理化学性质&存储条件

分子量	340.401
分子式	C17H16N4O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(3-carbamoyl-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)-1H-benzo[d]imidazole-5-carboxamide

参考文献

1. Clara Reglero, et al. Cancer Discov. 2022 Aug 19;CD-22-0010.

CRCD2 (NT5C2 inhibitor)

生物&药学活性

物理化学性质&存储条件

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CRCD2 (NT5C2 inhibitor)

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