Eltanexor Z-异构体（KPT-8602 Z-异构体）是 KPT-8602 活性较低的异构体。
| Cas No. | 1642300-78-4 |
| 别名 | KPT-8602 (Z-isomer) |
| Canonical SMILES | O=C(N)/C(C1=CN=CN=C1)=C\N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2 |
| 分子式 | C17H10F6N6O |
| 分子量 | 428.29 |
| 溶解度 | DMSO : 50 mg/mL (116.74 mM);Water :< 0.1 mg/mL (insoluble) |
| 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 | KPT-8602 Z-isomer is the less active isomer of KPT-8602. KPT-8602 is a potent CRM1 inhibitor.IC50:In Vitro: KPT 8602 Z-isomer exhibits different inhibitory effects on Z138, MM15, 3T3 cell lines, with IC50s of 100 nM-50 uM, 30 uM, respectively[1]. In Vivo: References:
[1]. Vercruysse T et al. The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia. Clin Cancer Res. 2016 Oct 25.
[2]. Hing ZA et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia. 2016 Jun 21.
[3]. Etchin J et al. KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia. 2016 Jun 24. |
