A Cdk7 inhibitor (IC50 = 13.9 nM); selective for Cdk7 over Cdk1

THZ2 – 50 mg

Brand:
Cayman
CAS:
1604810-84-5
Storage:
-20
UN-No:
Non-Hazardous - /

THZ2 is a Cdk7 inhibitor (IC50 = 13.9 nM) and a derivative of THZ1 (Item No. 9002215).{31733} It is selective for Cdk7 over Cdk1, -2, -5, -8, and -9 (IC50s = 96.9, 222, 134, 6,830, and 194 nM, respectively). THZ2 (0.001-1 nM) reduces proliferation of BT-549, HCC70, and MDA-MB-468 triple-negative breast cancer (TNBC) cells. In vivo, THZ2 (10 mg/kg) reduces tumor volume in an MDA-MB-231 mouse xenograft model. It also reduces tumor weight and volume, as well as the number of lung metastases, in an SJSA-1 osteosarcoma orthotopic mouse xenograft model.{58124}  

 

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SKU: 31055 - 50 mg Category:

Description

A Cdk7 inhibitor (IC50 = 13.9 nM); selective for Cdk7 over Cdk1, -2, -5, -8, and -9 (IC50s = 96.9, 222, 134, 6,830, and 194 nM, respectively); reduces proliferation of BT-549, HCC70, and MDA-MB-468 TNBC cells; reduces tumor volume in an MDA-MB-231 mouse xenograft model at 10 mg/kg; reduces tumor weight and volume, as well as the number of lung metastases, in an SJSA-1 osteosarcoma orthotopic mouse xenograft model

Formal name: N-[3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-3-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-benzamide

Synonyms: 

Molecular weight: 566.1

CAS: 1604810-84-5

Purity: ≥98%

Formulation: A solid

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