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MedChemExpressModel Mevociclib - 1816989-16-8

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Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors[1][2].
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Mevociclib

MCE China:Mevociclib

Brand:MedChemExpress (MCE)

Cat. No.HY-128587

CAS:1816989-16-8

Synonyms:SY-1365

Purity:99.27%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.

In Vitro:Mevociclib exhibits inhibition for CDK7/CycH/MAT1 with an IC50 of 20 nM[2].?Mevociclib is a highly selective covalent CDK7 inhibitor, induces apoptosis in leukemia cells, but not in non-malignant cells[2].?Mevociclib exhibits activity in breast, ovarian, colorectal and lung cancer cells that exhibited low nM EC50 and rapid induction of apoptosis[2].

In Vivo:Mevociclib (20mg/kg; i.v.; biw; for 35 days) inhibits tumor growth in TNBC in vivo models[2].?Mevociclib induces unique transcriptional signature[2].

IC50 & Target:CDK7

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References:

[1]. Hu S, et al. Discovery and characterization of SY-1365, a selective, covalent inhibitor of CDK7. Cancer Res. 2019 May 7.  [Content Brief]

[2]. Shanhu Hu, et al. SY-1365, a potent and selective CDK7 inhibitor, exhibits promising anti-tumor activity in multiple preclinical models of aggressive solid tumors.

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
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•   The biological activity of the products has been verified by the experiments of customers in various countries;
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