Ro 5-3335

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

Ro 5-3335是核心结合因子（CBF）抑制剂；使用 CBF 融合蛋白优先杀死人类白血病细胞系 (IC50 = 1.1 μM)。

Ro 5-3335 is core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). It represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. It also reduces the leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. It also is a Tat antagonist and inhibits HIV-1 replication in vitro.

Ro5-3335 has antiproliferative activity against human CBF leukemia cell lines, with IC50s 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.

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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Metabolic Enzyme/Protease

CETP

CBFβ-Runx1

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30195-30-3

259.69

C13H10ClN3O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (385.07 mM)

Clc1ccc2NC(=O)CN=C(c2c1)c3cccn3

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(-20℃)

With Ice Pack

≥ 2 years