HG-7-85-01|T38653|TargetMol

HG-7-85-01
1258391-13-7

￥10600 25mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP1年

联系人：邵小姐

手机：15002134094 拨打

邮箱：marketing@targetmol.cn

产品详情:

中文名称：: HG-7-85-01

英文名称：: HG-7-85-01

CAS号：: 1258391-13-7

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.

产品类别：: 抑制剂

货号：: T38653

Product Introduction

Bioactivity

名称	HG-7-85-01
描述	HG-7-85-01 is a type II ATP competitive inhibitor targeting wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. It effectively inhibits T315I mutant Bcr-Abl kinase, as well as KDR and RET kinases with IC50 values of 3 nM, 20 nM, and 30 nM, respectively. In contrast, HG-7-85-01 exhibits weak or no inhibition towards other kinases (IC50 >2 μM). Furthermore, this compound inhibits cell proliferation through the induction of apoptosis and by impeding cell-cycle progression.
体外活性	HG-7-85-01 (0-1 μM; 24 hours; BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells) treatment leads to G0G1 arrest of BCR-ABL-expressing cells[1]. HG-7-85-01 (0-1 μM; 72 hours; BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells) treatment also leads to induction of apoptosis of BCR-ABL-expressing cells[1]. HG-7-85-01 treatment potently and selectively inhibits the proliferation of 32D- and Ba/F3 cells expressing nonmutant BCR-ABL and the BCR-ABL-T315I gatekeeper mutant. HG-7-85-01 shows higher potency against nonmutant BCR-ABL and BCR-ABL-T315I (IC 50 = 0.06-0.14 μM)[1]. HG-7-85-01 inhibits BCR-ABL kinase activity in a concentration-dependent manner, suggesting selective targeting of the BCR-ABL kinase as the mechanism of action of HG-7-85-01[1]. HG-7-85-01 potently inhibits the proliferation of Ba/F3 cells expressing the Kit-T670I gatekeeper mutation (Ba/F3- Kit-T670I) and Ba/F3 cells expressing TEL/PDGFRβ and no effect on parental Ba/F3 cells. HG-7-85-01 inhibits Kit, PDGFR phosphorylation in a concentration-dependent manner[1]. The PDGFRα-T674M and PDGFRα-T674I gatekeeper mutant variants are highly responsive to HG-7-85-01 and significant IL-3 rescue[1]. HG-7-85-01 inhibits the proliferation of Ba/F3 cells transformed with human c-Src (EC 50 = 190 nM), T338I Src (EC 50 = 290 nM), and T338M Src (EC 50 = 150 nM; chicken c-Src numbering). And potently inhibits the proliferation of exon 11 Kit mutant-expressing cells, exon 9 kit mutant-expressing cells are significantly less responsive[1]. Cell Cycle Analysis[1]Cell Line: BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells Concentration: 0 μM, 0.01 μM, 0.1 μM and 1 μM Incubation Time: 24 hours Result: Led to G0G1 arrest of BCR-ABL-expressing cells. Apoptosis Analysis[1]Cell Line: BCR-ABL-, BCR-ABL-T315I-, Kit-T670I-, PDGFRα-T674M-, and PDGFRα-T674I-expressing cells Concentration: 0 μM, 0.01 μM, 0.1 μM and 1 μM Incubation Time: 72 hours Result: Led to induction of apoptosis of BCR-ABL-expressing cells.
体内活性	HG-7-85-01 has limited oral bioavailability (BAV % F mouse = 5 %, rat = 19 %), a moderate half life (T 1/2 mouse =1.1 h rat = 5.8 hours), a relative low maximal serum concentration (C max mouse = 106 ng/mL at 10 mg/kg , rat = 292 ng/mL and 2 mg/kg ) and a relatively high clearance (Cl mouse = 23 ml/min/kg, rat = 13 ml/min/kg)[1].
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
关键字	HG78501 \| HG-7-85-01 \| HG 7 85 01

HG-7-85-01|TargetMol

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	(12年)
注册资本	589.8595万人民币
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	中间体,天然产物,生物化工,化学试剂,生物技术服务

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