| Bioactivity | JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ∼250 and ∼500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia[1]. |
| Invitro | JI6 (3-1000 nM; 1-4 days) 以剂量依赖性方式抑制 MV4-11 细胞的活力，IC50 值为 ∼25 nM[1]。JI6 (1-2000 nM; 48 h) 有效抑制表达 FLT3-ITD，FLT3-D835Y 和 FLT3-D835H 的 HCD-57 细胞的活力，IC50 值为 ∼40 nM，对亲代 HCD-57 或表达 JAK2V617F 的细胞基本没有影响[1]。JI6 (100-500 nM; 24 h) 在表达 FLT3-ITD 和 FLT3-D835Y 的 HCD-57 细胞中诱导细胞凋亡和细胞周期停滞[1]。JI6 (50-500 nM; 3 h) 抑制表达 FLT3-ITD 和 FLT3-D835Y 的 HCD-57 细胞中 FLT3 及 ERK 和 Akt 的磷酸化[1]。 Cell Viability Assay[1] Cell Line: |
| In Vivo | JI6 (15 mg/kg; i.p. daily for 3 weeks) 抑制免疫缺陷小鼠体内表达 FLT3-D835Y 的 HCD-57 增殖并延长小鼠存活期[1]。JI6 (25 mg/kg; p.o. daily for 3 weeks) 抑制 FLT3-ITD 敲入小鼠的骨髓增生表型[1]。JI6 (100 mg/kg; a single i.p.) 在表达 FLT3-D835Y 的小鼠中显着抑制 FLT3 磷酸化和下游信号转导[1]。 Animal Model: |
| Name | JI6 |
| CAS | 856436-16-3 |
| Formula | C19H17N3O4S |
| Molar Mass | 383.42 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Chen Y, et, al. Identification of an orally available compound with potent and broad FLT3 inhibition activity. Oncogene. 2016 Jun 9;35(23):2971-8. |