1. Cell Cycle/DNA Damage JAK/STAT Signaling
  2. CDK Pim
  3. CDK2/PIM1-IN-1

CDK2/PIM1-IN-1 is an inhibitor of CDK2 (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM) kinases. CDK2/PIM1-IN-1 induces apoptosis and reduces tumor-promoting TNF-α expression. CDK2/PIM1-IN-1 has antitumor activity.

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CDK2/PIM1-IN-1 Chemical Structure

CDK2/PIM1-IN-1 Chemical Structure

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Description

CDK2/PIM1-IN-1 is an inhibitor of CDK2 (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM) kinases. CDK2/PIM1-IN-1 induces apoptosis and reduces tumor-promoting TNF-α expression. CDK2/PIM1-IN-1 has antitumor activity[1].

IC50 & Target[1]

CDK2

0.27 μM (IC50)

PIM1

0.67 μM (IC50)

In Vitro

CDK2/PIM1-IN-1 (Compound 6b) (24 h) shows antiproliferative effects on MCF7 cells (IC50: 5.54 μM), HCT-116 cells (IC50: 2.62 μM), HepG2 cells (IC50: 3.99 μM) and HeLa cell lines (IC50: 8.31 μM), with moderate safety in the normal breast cell line MCF-10A (IC50: 39.44 μM) [1].
CDK2/PIM1-IN-1 (24 h) inhibits HCT116 cell line at the G0-G1 phase (%G0-G1: 83.43%) and induced significant early (8.28%) and late (20.09%) cell apoptosis[1].
CDK2/PIM1-IN-1 (24 h) shows inhibitory effects on both CDK (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM) in HCT116 cell lines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Tumor cell line (MCF7 cells, HCT-116 cells, HepG2 cells, HeLa cell lines), and the normal breast cell line MCF-10A.
Concentration:
Incubation Time: 24 h
Result: Inhibited the cell viability of MCF7 cells (IC50: 5.54 μM), HCT-116 cells (IC50: 2.62 μM), HepG2 cells (IC50: 3.99 μM) and HeLa cell lines (IC50: 8.31 μM).
Showed moderate safety in the normal breast cell line MCF-10A (IC50: 39.44 μM).
In Vivo

CDK2/PIM1-IN-1 (Compound 6b) (10 mg/kg; IP; three times weekly for two weeks) reduces tumor volume (71.42%) and weight (70.58%) in the solid Ehrlich carcinoma (SEC) mouse model and was well tolerated. [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Solid Ehrlich carcinoma (SEC) mouse model[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), three times weekly for two weeks.
Result: Reduced tumor volume (71.42%) and weight (70.58%).
Showed good tolerability (indicated by stable body weight and 100% survival rate compared with the Dox-treated group).
Inhibited CDK2 (70.96%) and PIM1 (53.61%) levels in mouse tumors, tumor cell mitosis (27.35%).
Inhibited tumor TNF-α expression (17.61%).
Molecular Weight

421.49

Formula

C27H23N3O2

SMILES

COC1=CC=C(C2=CC=NC3=C2C(C4=CC=C(C)C=C4)=NN3C5=CC=CC=C5)C=C1OC

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Room temperature in continental US; may vary elsewhere.

Storage

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

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  • 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.

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Product Name:
CDK2/PIM1-IN-1
Cat. No.:
HY-173224
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