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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-G1T38 dihydrochloride
G1T38 dihydrochloride

Chemical Structure : G1T38 dihydrochloride

CAS No.: 2097938-59-3

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G1T38 dihydrochloride (Lerociclib)

货号: PC-60398Not For Human Use, Lab Use Only.

Lerociclib (G1T38) dihydrochloride is a potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

规格 价格 库存 数量
5 mg ￥1180 In stock
10 mg ￥1880 In stock
25 mg ￥2980 In stock
50 mg ￥4880 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Lerociclib (G1T38) dihydrochloride is a potent and selective inhibitor of CDK4/6 with biochemical IC50 of 1 nM and 2 nM for CDK4/cyclin D1 and CDK6/cyclin D3, respectively.
Lerociclib (G1T38) shows weak inhibitory effect on CDK9/cyclin T (IC50=28 nM) and CDK5/p35 (IC50=832 nM), >1,000-fold selectivity over CDK1/2/7.
Lerociclib (G1T38) decreases RB1 phosphorylation, causes G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines.
Lerociclib (G1T38) demonstrates equivalent or improved tumor efficacy compared to palbociclib in an ER+ breast cancer xenograft model.

物理化学性质&存储条件

分子量 547.529
分子式 C26H36Cl2N8O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2'-((5-(4-isopropylpiperazin-1-yl)pyridin-2-yl)amino)-7',8'-dihydro-6'H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one dihydrochloride

参考文献

1. Bisi JE, et al. Oncotarget. 2017 Jun 27;8(26):42343-42358.

2. Stice JP, et al. Mol Cancer Res. 2017 Jun;15(6):660-669.

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