Eltanexor

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种第二代 SINE、口服生物可利用的 Exportin 1 (XPO1、CRM1) 抑制剂。

A second-generation SINE, orally bioavailable Exportin 1 (XPO1,CRM1) inhibitor with markedly reduced brain penetration compared to selinexor (30-fold less); inhibits viability of human AML cell lines in vitro with IC50 of 20?211?nM, more active than the first-generation XPO1 inhibitor, selinexor; exhibits greater anti-leukemic efficacy against both leukemic blasts and LICs in AML patient-derived xenograft models, with no effect on normal hematopoietic stem and progenitor cell (HSPC) frequency.Blood Cancer Phase 2 Clinical.

Cell Viability Assay Cell Line:T-ALL cells (Jurkat, MOLT-4, ALL-SIL, DND41, and HPB-ALL), B-ALL cells (BV173, EHEB, and REH), AML cells (MV4-11, MOLM13, K-562, and HL-60)Concentration:2, 4, 6 nM Incubation Time:72 hours Result:Cell viability was reduced with EC50 values ranging from 25 to 145 nM.Western Blot Analysis Cell Line:T-ALL, B-ALL, AML cells Concentration:1 μM Incubation Time:16 hours Result:Appearance of cleaved caspase-3 substrate PARP as early as 6 hours.

Animal Model:Female BALB/c mice (model with the JAK3 (M511I) mutation)Dosage:15 mg/kgAdministration:Oral gavage; daily for 12 daysResult:Showed a marked reduction in total white blood cell (WBC) counts after 2 days of treatment compared to placebo-treated animals and the WBC counts continued to drop until they reached normal levels (<10,000 cells/μL) by day 12.

KPT-8602 | KPT8602

Membrane Transporter/Ion Channel

Exportin-1

Exportin-1

Cancer

Blood cancer

1642300-52-4

428.2913

C17H10F6N6O

>98% (HPLC)

DMSO: 4.72 mg/mL

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

5-Pyrimidineacetamide, α-[[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]methylene]-, (αE)-

(-20℃)

With Ice Pack

≥ 2 years