CDK6/PIM1-IN-1
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity.
For research use only. We do not sell to patients.
- CAS No.: 2677026-14-9
- Formula: C25H28FN9
- Molecular Weight:473.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CDK6/cyclinD1 39 nM (IC50) |
CDK1/cyclinB >10 μM (IC50) |
CDK2/cyclinA 2.274 μM (IC50) |
CDK3/Cyclin E >10 μM (IC50) |
Cdk4/cyclin D1 3.6 nM (IC50) |
Cdk5/p25 >10 μM (IC50) |
CDK7/Cyclin H/MNAT1 393 nM (IC50) |
CDK9/cyclinT1 440 nM (IC50) |
CDK12/Cyclin K >10 μM (IC50) |
CDK13/Cyclin K >10 μM (IC50) |
PIM1 88 nM (IC50) |
PIM2 >10 μM (IC50) |
PIM3 92 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | GI50 |
1.07 μM
Compound: 51
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Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
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[PMID: 34958208] |
| K562 | GI50 |
1.03 μM
Compound: 51
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Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
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[PMID: 34958208] |
| MOLM-13 | GI50 |
1.362 μM
Compound: 51
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Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
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[PMID: 34958208] |
| Mononuclear cell line | GI50 |
5.33 μM
Compound: 51
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Antiproliferative activity against AML patient derived mononuclear cells of assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
Antiproliferative activity against AML patient derived mononuclear cells of assessed as cell growth inhibition incubated for 72 hrs by CCK8 assay
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[PMID: 34958208] |
CDK6/PIM1-IN-1 (compound 51) exhibits more than 10 times selectivity over CDK1 (IC50>10 μM), CDK2 (IC50=2.274 μM), CDK3 (IC50>10 μM), CDK5 (IC50>10 μM), CDK7 (IC50=393 nM), CDK9 (IC50=440 nM), CDK12 (IC50>10 μM), and CDK13 (IC50>10 μM). CDK6/PIM1-IN-1 shows inhibitory activity against PIM2 (IC50>10 μM) and PIM3 (IC50=92 nM)[1].
CDK6/PIM1-IN-1 inhibits proliferation in AML cells (K562 cell,GI50=1.026 μM; HL-60 cell,GI50=1.069 μM; MOLM13 cell, GI50=1.362 μM)[1].
CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM) causes a G1 arrest in a dose-dependent manner in K562 and HL-60 cell lines[1].
CDK6/PIM1-IN-1 (1, 2, 4 μM) promotes the apoptosis of K562 and HL-60 cell lines in a dose-dependent manner[1].
CDK6/PIM1-IN-1 (0.5, 1, 1.5 μM; for 24 h) reduces p-retinoblastoma (RB) and p-BAD levels in a concentration-dependent manner. CDK6/PIM1-IN-1 decreases the PIM1 level[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CDK6/PIM1-IN-1 (iv; 5 mg/kg) has the t1/2, MRT0-∞, and AUC0-∞ values of 9.78 h, 14.61 h, and 1153.74 h·ng/mL, respectively in Sprague-Dawley (SD) rats[1].
CDK6/PIM1-IN-1 (po; 5 mg/kg) has the t1/2, Tmax, Cmax, and AUC0-∞ of 15.81 h, 11 h, 152.31 ng/mL, and 5152.92 h·ng/mL, respectively in SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2677026-14-9
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Molecular Weight 473.55
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Formula C25H28FN9
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SMILES
FC1=CN=C(NC2=NC=C(N3CCNCC3)C=C2)N=C1C4=CC=C5N=CC(N(CC)CC)=NC5=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK6/PIM1-IN-1 Related Classifications
HY-142696 Related Classifications
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