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Chemical Structure : CRCD2
Catalog No.: 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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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.
| M.Wt | 340.401 | |
| Formula | C17H16N4O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Clara Reglero, et al. Cancer Discov. 2022 Aug 19;CD-22-0010.
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