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THZ1-R

Names

[ CAS No. ]:
1621523-07-6

[ Name ]:
THZ1-R

[Synonym ]:
Benzamide, N-[3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-4-[[4-(dimethylamino)-1-oxobutyl]amino]-
N-(3-{[5-Chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino}phenyl)-4-{[4-(dimethylamino)butanoyl]amino}benzamide

Biological Activity

[Description]:

THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.

[Related Catalog]:

Research Areas >> Cancer

[Target]

CDK7:146 nM (IC50)


[In Vitro]

THZ1-R shows lower affinity at CDK7 than THZ1, with IC50 of 146 nM[1].

[Cell Assay]

Cells are seeded in 384-well microplates at 15% confluency in medium with 5% FBS and penicillin/streptavidin. Cells are treated with THZ1 or DMSO for 72 hrs and cell viability is determined using resazurin.

[References]

[1]. Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20.


[Related Small Molecules]

Abemaciclib(LY2835219) | Ribociclib (LEE011) | Dinaciclib (SCH727965) | THZ1 2HCl | Roscovitine (CYC202) | THZ531 | RO-3306 | Flavopiridol | NVP 2 | BAY-1143572 Racemate | CYC-065 | AZD5438 | BIO | Kenpaullone | SNS-032 (BMS-387032)

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C31H30ClN7O2

[ Molecular Weight ]:
568.069

[ Exact Mass ]:
567.214966

[ LogP ]:
4.70

[ Index of Refraction ]:
1.720

[ Storage condition ]:
2-8℃

Related Compounds