CDK-IN-2|cas 1269815-17-9|DC Chemicals

Cas No.:	1269815-17-9
Chemical Name:	Piperidine-3-carboxylic acid [5-chloro-4-(5-fluoro-2-methoxy-phenyl)-pyridin-2-yl]-amide
Synonyms:	Piperidine-3-carboxylic acid [5-chloro-4-(5-fluoro-2-methoxy-phenyl)-pyridin-2-yl]-amide;(3R)-N-[5-chloro-4-(5-fluoro-2-methoxyphenyl)pyridin-2-yl]piperidine-3-carboxamide;CDK inhibitor II;(R)-N-(5-chloro-4-(5-fluoro-2-methoxyphenyl)pyridin-2-yl)piperidine-3-carboxamide trifluoroacetate;(R)-piperidine-3-carboxylic acid [5-chloro-4-(5-fluoro-2-methoxyphenyl)-pyridin-2-yl]-amide;CS-0239;HY-13033;SureCN1438999;(3R)-N-[5-Chloro-4-(5-fluoro-2-methoxyphenyl)-2-pyridinyl]-3-piperidinecarboxamide;CDK-IN-2
SMILES:	FC1=CC(C2=CC(NC([C@H]3CNCCC3)=O)=NC=C2Cl)=C(C=C1)OC
Formula:	₃₆₄
M.Wt:	C18H19ClFN3O2
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM.
Target:	CDK9/cyclinT1:8 nM (IC50)
References:	[1]. Keith B Pfister, et al. Heteroaryl compounds as kinase inhibitors. 2011, WO2011026917A1.

Cat. No.	Product name	Field of application
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DC73181	XPW1	XPW1 is a potent and selective CDK9 inhibitor with excellent anti-ccRCC activity and low toxicity.
DC73178	SNX631	SNX631 (SNX-631) is a potent, selective inhibitor of CDK8/19 Mediator kinase with IC50 of 10.3 nM in the NF κB-dependent cell-based assays.
DC73175	NCGC00131308	NCGC00131308 is a small molecule inhibitor that effectively disrupts IQGAP1-Cdc42 interaction in breast cancer cells, shows EC50 of 4.47 uM in biochemical HTRF assays.
DC73171	ISM042-2-048	ISM042-2-048 is a potent, selective inhibitor of cyclin-dependent kinase 20 (CDK20, cell cycle-related kinase/CCRK) with IC50 of 33.4 nM (CDK20/CycT1), Kd value of 566 nM.
DC73170	GFH009	GFH009 is a potent, selective CDK9 inhibitor, inhibits the activity of the CDK9/cyclin T1 regulatory complex of P-TEFb.
DC70984	(S)-CR8	(S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM).
DC70766	Senexin C	Senexin C is a novel potent, selective and orally bioavailable CDK8/19 inhibitor with Kd of 1.4 and 2.9 nM for CDK8/CycC and CDK19/CycC, respectively.Senexin C inhibits CDK8/CycC with IC50 of 3.6 nM, shows high selectivity against other HDAC isoforms.Senexin C is more metabolically stable and provides a more sustained inhibition of CDK8/19-dependent cellular gene expression when compared with the prototype inhibitor Senexin B.Senexin C inhibits MV4-11 leukemia growth in a systemic in vivo model with good tolerability.
DC70298	CDDD11-8	CDDD11-8 is a potent CDK9 inhibitor co-targeting FLT3-ITD with Ki values of 8 and 13 nM, respectively.CDDD11-8 displays excellent kinome selectivity in a panel of 369 human kinases.CDDD11-8 displays antiproliferative activity against leukemia cell lines, and particularly potent effects against MV4-11 and MOLM-13 cells, which are known to harbor the FLT3-ITD mutation and mixed lineage leukemia (MLL) fusion proteins.CDDD11-8 causes a robust tumor growth inhibition by oral administration in animal xenografts, induces tumor regression at dose of 125 mg/kg.
DC70230	AZ5576	AZ5576 (AZ-5576) is a potent, selective CDK9 inhibitor with an IC 50 <5 nM, decreases phosphorlyation of Ser2-RNAPII in cells with an IC 50 of 96 nM.AZ5576 downregulated Mcl-1 and MYC protein abundance across multiple tested DLBCL cell lines and in primary DLBCL cells.MYC sensitizes DLBCL cells to AZ5576, genetic downregulation of MYC in U-2932 and OCI-LY19 cells resulted in diminished susceptibility to AZ5576.AZ5576 dose-dependently downregulated MYC transcription of a luciferase reporter containing multiple canonical MYC-MAX-binding sites, an effect more pronounced compared with multi-CDK inhibitor dinaciclib.AZ5576 restricts growth of xenografted DLBCL tumors in vivo.