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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-SY-1365
SY-1365

Chemical Structure : SY-1365

CAS No.: 1816989-16-8

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SY-1365 (Mevociclib, SY1365)

货号: PC-72642Not For Human Use, Lab Use Only.

SY-1365 (Mevociclib, SY1365) is a potent, selective, covalent CDK7 inhibitor with Ki of 17.4 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SY-1365 (Mevociclib, SY1365) is a potent, selective, covalent CDK7 inhibitor with Ki of 17.4 nM.
SY-1365 displayed high selectivity against all other CDKs including CDK2,9 and 12 (IC50>2 uM), and 8 of 468 kinases including CDK7 were inhibited >90% in the kinome screen (DiscoverX KINOMEscan) at 1 uM.
SY-1365 dose- and time-dependently inhibited CDK7 substrates including RNAPII CTD phosphorylation at Ser2/5/7 sites and Thr160 of CDK2, caused massive cell death at 100 and 250 nM SY-1365 24 and 48 hours treatment in THP1, HCC70, and RPE-hTERT cell lines.
SY-1365 induced apoptosis in AML and TNBC cell lines but not in immortalized normal cell lines.
SY-1365 showed significant growth inhibition and cell killing in 386 human cell lines representing 26 cancer types in nanomolar range.
SY-1365 demonstrated substantial antitumor effects in multiple AML xenograft models as a single agent.
SY-1365-induced growth inhibition was enhanced in combination with the BCL2 inhibitor venetoclax.
SY-1365 is more potent, selective, and metabolically stable than THZ1.

物理化学性质&存储条件

分子量 587.125
分子式 C31H35ClN8O2
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 (5.9 mg/mL)
Chemical Name/SMILES

N-((1S,3R)-3-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)-1-methylcyclohexyl)-5-((E)-4-(dimethylamino)but-2-enamido)picolinamide

参考文献

1. Hu S, et al. Cancer Res. 2019 Jul 1;79(13):3479-3491.

2. Webb BM, et al. J Biol Chem. 2021 Oct;297(4):101162.

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