IIIM-290

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IIIM-290 is a potent and oral CDK inhibitor with IC₅₀s of 90 and 94 nM for CDK2/A and CDK9/T1.

For research use only. We do not sell to patients.

IIIM-290 Chemical Structure

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•Related Small Molecules:

•Related Proteins:

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View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

IIIM-290 is a potent and oral CDK inhibitor with IC₅₀s of 90 and 94 nM for CDK2/A and CDK9/T1.

IC₅₀ & Target^[1]

CDK2/A

90 nM (IC₅₀)

CDK9/T1

94 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	GI₅₀	6 μM Compound: 11d	Growth inhibition of human 786-0 cells after 48 hrs by MTT assay Growth inhibition of human 786-0 cells after 48 hrs by MTT assay	[PMID: 29370702]
A-431	GI₅₀	8 μM Compound: 11d	Growth inhibition of human A431 cells after 48 hrs by MTT assay Growth inhibition of human A431 cells after 48 hrs by MTT assay	[PMID: 29370702]
A549	GI₅₀	4 μM Compound: 11d	Growth inhibition of human A549 cells after 48 hrs by MTT assay Growth inhibition of human A549 cells after 48 hrs by MTT assay	[PMID: 29370702]
BT-549	GI₅₀	5 μM Compound: 11d	Growth inhibition of human BT549 cells after 48 hrs by MTT assay Growth inhibition of human BT549 cells after 48 hrs by MTT assay	[PMID: 29370702]
Caco-2	GI₅₀	7 μM Compound: 11d	Growth inhibition of human Caco2 cells after 48 hrs by MTT assay Growth inhibition of human Caco2 cells after 48 hrs by MTT assay	[PMID: 29370702]
COLO 205	GI₅₀	7 μM Compound: 11d	Growth inhibition of human COLO205 cells after 48 hrs by MTT assay Growth inhibition of human COLO205 cells after 48 hrs by MTT assay	[PMID: 29370702]
DU-145	GI₅₀	5 μM Compound: 11d	Growth inhibition of human DU145 cells after 48 hrs by MTT assay Growth inhibition of human DU145 cells after 48 hrs by MTT assay	[PMID: 29370702]
HCT-116	GI₅₀	5 μM Compound: 11d	Growth inhibition of human HCT116 cells after 48 hrs by MTT assay Growth inhibition of human HCT116 cells after 48 hrs by MTT assay	[PMID: 29370702]
HEK293	IC₅₀	> 50 μM Compound: 11d	Inhibition of [3H]-astemizole binding to human ERG expressed in HEK293 cell membranes by scintillation counting method Inhibition of [3H]-astemizole binding to human ERG expressed in HEK293 cell membranes by scintillation counting method	[PMID: 29370702]
HEK293	GI₅₀	22 μM Compound: 11d	Growth inhibition of human HEK293 cells after 48 hrs by MTT assay Growth inhibition of human HEK293 cells after 48 hrs by MTT assay	[PMID: 29370702]
HL-60	GI₅₀	0.9 μM Compound: 11d	Growth inhibition of human HL60 cells after 48 hrs by MTT assay Growth inhibition of human HL60 cells after 48 hrs by MTT assay	[PMID: 29370702]
HOP-62	GI₅₀	7 μM Compound: 11d	Growth inhibition of human HOP62 cells after 48 hrs by MTT assay Growth inhibition of human HOP62 cells after 48 hrs by MTT assay	[PMID: 29370702]
HOP-92	GI₅₀	3 μM Compound: 11d	Growth inhibition of human HOP92 cells after 48 hrs by MTT assay Growth inhibition of human HOP92 cells after 48 hrs by MTT assay	[PMID: 29370702]
LOX IMVI	GI₅₀	4 μM Compound: 11d	Growth inhibition of human LOXIMVI cells after 48 hrs by MTT assay Growth inhibition of human LOXIMVI cells after 48 hrs by MTT assay	[PMID: 29370702]
MCF7	GI₅₀	4 μM Compound: 11d	Growth inhibition of human MCF7 cells after 48 hrs by MTT assay Growth inhibition of human MCF7 cells after 48 hrs by MTT assay	[PMID: 29370702]
MDA-MB-231	GI₅₀	4 μM Compound: 11d	Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 29370702]
MDA-MB-468	GI₅₀	4 μM Compound: 11d	Growth inhibition of human MDA-MB-468 cells after 48 hrs by MTT assay Growth inhibition of human MDA-MB-468 cells after 48 hrs by MTT assay	[PMID: 29370702]
MIA PaCa-2	GI₅₀	1 μM Compound: 11d	Growth inhibition of human MIAPaCa2 cells after 48 hrs by MTT assay Growth inhibition of human MIAPaCa2 cells after 48 hrs by MTT assay	[PMID: 29370702]
MOLT-4	GI₅₀	0.5 μM Compound: 11d	Growth inhibition of human MOLT4 cells after 48 hrs by MTT assay Growth inhibition of human MOLT4 cells after 48 hrs by MTT assay	[PMID: 29370702]
NCI-H226	GI₅₀	4 μM Compound: 11d	Growth inhibition of human NCI-H226 cells after 48 hrs by MTT assay Growth inhibition of human NCI-H226 cells after 48 hrs by MTT assay	[PMID: 29370702]
NCI-H522	GI₅₀	5 μM Compound: 11d	Growth inhibition of human NCI-H522 cells after 48 hrs by MTT assay Growth inhibition of human NCI-H522 cells after 48 hrs by MTT assay	[PMID: 29370702]
OVCAR-3	GI₅₀	8 μM Compound: 11d	Growth inhibition of human OVCAR3 cells after 48 hrs by MTT assay Growth inhibition of human OVCAR3 cells after 48 hrs by MTT assay	[PMID: 29370702]
OVCAR-4	GI₅₀	9 μM Compound: 11d	Growth inhibition of human OVCAR4 cells after 48 hrs by MTT assay Growth inhibition of human OVCAR4 cells after 48 hrs by MTT assay	[PMID: 29370702]
OVCAR-5	GI₅₀	7 μM Compound: 11d	Growth inhibition of human OVCAR5 cells after 48 hrs by MTT assay Growth inhibition of human OVCAR5 cells after 48 hrs by MTT assay	[PMID: 29370702]
PANC-1	GI₅₀	4 μM Compound: 11d	Growth inhibition of human PANC1 cells after 48 hrs by MTT assay Growth inhibition of human PANC1 cells after 48 hrs by MTT assay	[PMID: 29370702]
PC-3	GI₅₀	3 μM Compound: 11d	Growth inhibition of human PC3 cells after 48 hrs by MTT assay Growth inhibition of human PC3 cells after 48 hrs by MTT assay	[PMID: 29370702]
T47D	GI₅₀	6 μM Compound: 11d	Growth inhibition of human T47D cells after 48 hrs by MTT assay Growth inhibition of human T47D cells after 48 hrs by MTT assay	[PMID: 29370702]

Molecular Weight

462.32

Formula

C₂₃H₂₁Cl₂NO₅

CAS No.

2213468-64-3

SMILES

OC1=C2C(OC(/C=C/C3=C(Cl)C=CC=C3Cl)=CC2=O)=C([C@]4([H])[C@H](O)CN(C)CC4)C(O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Bharate SB, et al. Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor. J Med Chem. 2018 Feb 22;61(4):1664-1687. [Content Brief]

IIIM-290 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IIIM-2902213468-64-3IIIM290IIIM 290CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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