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OT-82

CAS No. : 1800487-55-1

MCE 国际站：OT-82

产品活性：OT-82 是一种强效、选择性和具有口服活性的 NAMPT 的抑制剂。OT-82 对造血源细胞有选择性毒性，以 NAD⁺ 依赖方式诱导细胞死亡。OT-82 是一种很有前途的抗肿瘤试剂 (antineoplastic agent)，用于血液系统恶性肿瘤的研究。

研究领域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：NAMPT  |  Caspase

In Vitro: OT-82 (0.0001-10 μM; 72 hours) demonstrates tissue-selective (HP vs non-HP) cytotoxicity. It is against HP cell lines MV4–11, U937, RS4;11, HEL92.1.7 and PER485 cell growth with IC₅₀ values of 2.11 nM, 2.70 nM, 1.05 nM and 1.36 nM, respectively. It also against nonHP cell lines MCF-7, U87, HT29, and H1299 cell growth with IC₅₀ values of 37.92 nM, 29.52 nM, 15.67 nM and 7.95 nM , respectively.
OT-82 demonstrates cancer-selective (tumor vs normal) cytotoxicity. It more sensitive to BMMNC from leukemia patients, the IC₅₀ values are 31 nM and 7.10 nM for AML and ALL donors, respectively. The IC₅₀ value is 62.69 nM for BMMNC from healthy donors.
OT-82 (0.001-10 μM; 48 hours) inhibits recombinant NAMPT activity and causes dose-dependent reductions in cellular NAD and ATP concentrations in MV4–11 cells.
OT-82 (0.01-100 nM; 48 hours) results in activation of caspase-3, an increase in the proportion of cells with sub-G1 DNA content, and depolarization of the mitochondrial membrane in MV4–11 cells.

In Vivo: OT-82 (oral gavage; 20 or 40 mg/kg; 3 weeks) treatment increases survival to 100% and 56% at 40 or 20 mg/kg, respectively after treatment discontinuation in SC xenograft model of Burkitt's lymphoma.

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