Forodesine hydrochloride (BCX-1777) (BCX-1777 hydrochloride) 是一种高效且具有口服活性的嘌呤核苷磷酸化酶 (PNP) 抑制剂,对人、小鼠、大鼠、猴子和狗 PNP 的 IC50 值为 0.48 至 1.57 nM。 Forodesine hydrochloride (BCX-1777) 是一种有效的人类淋巴细胞增殖抑制剂。 Forodesine hydrochloride (BCX-1777) 可通过增加 dGTP 水平诱导白血病细胞凋亡。
Cas No. | 284490-13-7 |
别名 | BCX-1777 hydrochloride; Immucillin-H hydrochloride |
Canonical SMILES | O=C1C(NC=C2[C@@H]3N[C@H](CO)[C@@H](O)[C@H]3O)=C2NC=N1.Cl |
分子式 | C11H15ClN4O4 |
分子量 | 302.71 |
溶解度 | Water : ≥ 74.1 mg/mL (244.79 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Forodesine hydrochloride is a potent and oral purine nucleoside phosphorylase (PNP) inhibitor with IC50s ranging from 0.48 to 1.57 nM. [1]. Homminga I, et al. In vitro efficacy of forodesine and nelarabine (ara-G) in pediatric leukemia. Blood. 2011 Aug 25;118(8):2184-90. [2]. Ogura M, et al. Phase I study of BCX1777 (forodesine) in patients with relapsed or refractory peripheral T/natural killer-cell malignancies. Cancer Sci. 2012 Jul;103(7):1290-5. [3]. Bieghs L, et al. The effects of forodesine in murine and human multiple myeloma cells. Adv Hematol. 2010;2010:131895. [4]. Yamauchi T, et al. A nelarabine-resistant T-lymphoblastic leukemia CCRF-CEM variant cell line is cross-resistant to the purine nucleoside phosphorylase inhibitor forodesine. Anticancer Res. 2014 Sep;34(9):4885-92. |