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  • PLX647 dihydrochloride|T39194|TargetMol

PLX647 dihydrochloride|T39194|TargetMol

PLX647 dihydrochloride
1779796-38-1
10600 25mg 起订
上海 更新日期:2025-11-17

TargetMol中国(陶术生物)

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联系人:邵小姐
手机:4008200310 拨打
邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
PLX647 dihydrochloride
英文名称:
PLX647 dihydrochloride
CAS号:
1779796-38-1
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
产品类别:
抑制剂
货号:
T39194

Product Introduction

Bioactivity

名称PLX647 dihydrochloride
描述PLX647 dihydrochloride is a potent and selective dual inhibitor of FMS and KIT kinases, with IC50 values of 28 nM and 16 nM, respectively. At a concentration of 1 μM, PLX647 dihydrochloride demonstrates superior selectivity against a wide range of 400 kinases, except FLT3 and KDR, where IC50 values are 91 nM and 130 nM, respectively. This orally active compound holds great potential for targeted kinase inhibition.
体外活性In vitro, PLX647 dihydrochloride potently inhibits proliferation of BCR-FMS cells, with an IC 50 of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647 dihydrochloride, with an IC 50 of 180 nM. PLX647 dihydrochloride also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC 50 =380 nM) and M-07e (IC 50 =230 nM), which express FMS and KIT, respectively[1]. PLX647 dihydrochloride potently inhibits the growth of FLT3-ITD-expressing MV4-11 cells (IC 50 =110 nM). PLX647 dihydrochloride displays minimal inhibition of the proliferation of Ba/F3 cells expressing BCR-KDR (IC 50 =5 μM). PLX647 dihydrochloride inhibits osteoclast differentiation with an IC 50 of 0.17 μM[1].
体内活性PLX647 dihydrochloride (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes[1]. PLX647 dihydrochloride (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release[1]. PLX647 dihydrochloride (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis[1]. PLX647 dihydrochloride (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 dihydrochloride (30 mg/kg BID) is able to prevent bone damage by the tumor cells[1]. Animal Model: Male C57BL/6 mice (mouse unilateral ureter obstruction model)[1]Dosage: 40 mg/kg Administration: P.o.; twice daily for 7 days Result: Resulted in reduction in the levels of F4/80+ macrophages by 77%. Animal Model: 7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model)[1]Dosage: 20 mg/kg, 80 mg/kg Administration: P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days Result: 20 mg/kg PLX647 had no initial effect on the development of severe arthritis. However, starting on day 33, no further development of disease severity was recorded, and a 30% inhibition of the macroscopic signs of arthritis was evident in clinical score on day 41. Mice treated with 80 mg/kg BID PLX647 initially shows delayed development of severe arthritic signs. Starting on day 33, the signs of arthritis began to decrease in this treatment group, reaching a maximum reversal of 76% on day 41.
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
关键字PLX-647 Dihydrochloride | PLX-647 dihydrochloride | PLX647 Dihydrochloride | PLX647 dihydrochloride | PLX-647 | PLX647 | PLX 647 Dihydrochloride | PLX 647
相关产品Gilteritinib | Axitinib | Sorafenib tosylate | Lenvatinib mesylate | Regorafenib | Dasatinib | Pazopanib | Sorafenib | Imatinib Mesylate | Pexidartinib | Sunitinib | Regorafenib monohydrate
PLX647 dihydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (13年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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