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Cat. No.: HY-111356

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IIIM-290

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.

CAS No.: 2213468-64-3
Formula: C₂₃H₂₁Cl₂NO₅
Molecular Weight:462.32

Storage:

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

Data Sheet (271 KB)

IIIM-290 Chemical Structure

CAS No.: 2213468-64-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

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)

All CDK Isoforms :

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]
HCT-116	GI₅₀	9.32 μM Compound: 1e; IIIM-290	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37302342]
HEK293	GI₅₀	>100 μM Compound: 1e; IIIM-290	Antiproliferative activity against HEK293 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against HEK293 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37302342]
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]
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]
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]
MIA PaCa-2	GI₅₀	1.94 μM Compound: 1e; IIIM-290	Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human MIA PaCa-2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 37302342]
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]

Chemical Information

CAS No. 2213468-64-3
Molecular Weight 462.32
Formula C₂₃H₂₁Cl₂NO₅
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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