CDK12 inhibitor E9 S-isomer|E9;CDK12-IN-E9

Cas No.:	2020052-55-3
Chemical Name:	(S)-N-(3-((3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)phenyl)acrylamide
Synonyms:	E9;CDK12-IN-E9
SMILES:	C(NC1=CC=CC(NC2N3N=CC(CC)=C3N=C(N3CCCC[C@@H]3CCO)C=2)=C1)(=O)C=C
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

CDK12 inhibitor E9 S-isomer (E9, CDK12-IN-E9) is a clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux; dose-dependently decreases phosphorylated and total RNAPII in THZ1R NB and lung cancer models, competed strongly with bio-THZ1 for binding to CDK12 at low nanomolar ranges, but not CDK7 (>1 uM); exerts its cytotoxic effects through covalent modification of cysteine 1039 of CDK12; shows more potent antiproliferative activity in THZ1R NB and lung cancer cells with IC50 ranging from 8 to 40 nM than ribociclib, palbociclib, and AZD5438.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47707	CDK/HDAC-IN-1	CDK/HDAC-IN-1 shows remarkable CDK2/4/6 and HDAC6 inhibitory activity of IC50 = 60.9 ± 2.9, 276 ± 22.3, 27.2 ± 4.2, and 128.6 ± 0.4 nM, respectively.
DC47706	CDK2-IN-7	CDK2-IN-7 is a CDK2 inhibitor for treating cancer (IC50 < 50 nM).
DC47705	JH-XVI-178	JH-XVI-178 is a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties.
DC47704	CDK9-IN-12	CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.
DC47236	Cirtuvivint	Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research.
DC47205	Eltenac	Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood.
DC47130	CDK5-IN-1	CDK5-IN-1, a potent CDK5 inhibitor, is against CDK5 activity less than 10 nM. CDK5-IN-1 is used for kidney diseases research.
DC47109	Cimpuciclib	Cimpuciclib is a cyclin-dependent kinase(CDK) inhibitor and antineoplastic.
DC47043	Ocarocoxib	Ocarocoxib, a potent COX-2 (cyclooxygenase-2) inhibitor, is a non-steroidal anti-inflammatory for veterinary use.
DC46945	Avotaciclib	Avotaciclib (BEY1107) is an orally active cyclin dependent kinase 1 (CDK1) inhibitor. Avotaciclib can be used for the research of cancer.