中文名 | 7-氯-5-(1H-吡咯-2-基)-1H-苯并[e][1,4]二氮杂卓-2(3H)-酮 |
英文名 | Ro 5-3335 |
别名 | 化合物RO 5-3335 7-氯-5-(1H-吡咯-2-基)-1H-苯并[e][1,4]二氮杂卓-2(3H)-酮 |
英文别名 | NSC-66020 Ro 5-3335 CBFβ-Runx1 inhibitor II 7-Chloro-5-(1H-pyrrol-2-yl)-1H-benzo[e][1,4]diazepin-2(3H)-one 7-Chloro-1,3-dihydro-5-(1H-pyrrol-2-yl)-2H-1,4-benzodiazepin-2-one 7-Chloro-5-(1H-pyrrol-2-yl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one 7-Chloro-2-oxo-5-(1H-pyrrol-2-yl)-2,3-dihydro-1H-1,4-benzodiazepine 2H-1,4-Benzodiazepin-2-one, 7-chloro-1,3-dihydro-5-(1H-pyrrol-2-yl)- |
CAS | 30195-30-3 |
化学式 | C13H10ClN3O |
分子量 | 259.69 |
密度 | 1.46 g/cm3 |
熔点 | 256 °C(dec.) |
沸点 | 501.6 °C at 760 mmHg |
闪点 | 257.1 °C |
存储条件 | 2-8℃ |
外观 | 微浅黄色至浅红黄色晶体或粉末 |
MDL号 | MFCD00870704 |
体外研究 | Ro5-3335 has antiproliferative activity against human CBF leukemia cell lines, with IC 50 s of 1.1 μM, 21.7 μM and 17.3 μM for ME-1, Kasumi-1 and REH, respectively. Ro5-3335 inhibits definitive hematopoiesis in zebrafish embryos. Ro5-3335 does not completely break apart RUNX1-CBFβ interaction, but changes the conformation of their complex or increases the distance between RUNX1 and CBFβ in the complex. |
体内研究 | Ro5-3335 is identified as an inhibitor of RUNX1–CBFβ function in zebrafish models. Ro5-3335 rescues preleukemic phenotype in a RUNX1-ETO transgenic zebrafish. Ro5-3335 (300 mg/kg/d; p.o; for 30 days) reduces leukemia burden in a mouse CBFB-MYH11 leukemia model. Animal Model: C57BL/6 mice (leukemic model) Dosage: 300 mg/kg Administration: Oral administration; daily; for 30 days Result: Reduced the number of c-kit + cells in the transplanted mice and leukemic cell infiltration in the livers, bone marrow and spleen. |
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