NU6027 是一种有效且的、ATP竞争性的 CDK1 和 CDK2 的抑制剂，K_i 值分别为 2.5 µM 和 1.3 µM。NU6027 也是 ATR 的有效抑制剂，以 ATR 依赖性方式增强羟基脲和顺铂的细胞毒性。

NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with K i s of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.

Solid

CDK1 2.5 μM (Ki) CDK2 1.3 μM (Ki)

NU6027 (1 nM-100 μM; 48 h) inhibits the growth of human tumor cells with a GI50 of 10±6 μM.
NU6027 (0.1-25 μM; 24 h) inhibits ATR activity with an IC50 of 2.8 μM in GM847KD cells. NU6027 (1-10 μM; 24 h) inhibits ATR activity with an IC50 of 6.7±2.3 μM in MCF7 cells.
NU6027 (4 or 10 μM; 24 h) attenuates G2/M arrest following DNA damage in MCF7 cells.
NU6027 (10 μM; 24 h) significantly reduces RAD51 foci in both control and PF-01367338-treated V-C8 B2 cells.
NU6027 (4 μM; 24 h) causes 82% suppression of the increase in RAD51 foci-positive cells treated by PF-01367338. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Arris CE, et, al. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem. 2000 Jul 27; 43(15): 2797-804.
[2]. Peasland A, et, al. Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines. Br J Cancer. 2011 Jul 26;105(3):372-81.

In Vitro: DMSO : 12.5 mg/mL (49.75 mM; ultrasonic and warming and heat to 60°C)配制储备液