1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. CDK Carbonic Anhydrase
  3. CDK2-IN-12

CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity.

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CDK2-IN-12 Chemical Structure

CDK2-IN-12 Chemical Structure

CAS No. : 2410402-88-7

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Description

CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity[1].

IC50 & Target

CDK2

11.6 μM (IC50)

CDK9

>12.5 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
15.1 μM
Compound: 10b
Antiproliferative activity against human MCF7 cells measured after 48 hrs under CoCl2-induced hypoxic condition by MTT assay
Antiproliferative activity against human MCF7 cells measured after 48 hrs under CoCl2-induced hypoxic condition by MTT assay
[PMID: 31972394]
MCF7 IC50
6.8 μM
Compound: 10b
Antiproliferative activity against human MCF7 cells measured after 48 hrs under normoxic condition by MTT assay
Antiproliferative activity against human MCF7 cells measured after 48 hrs under normoxic condition by MTT assay
[PMID: 31972394]
MDA-MB-468 IC50
1.37 μM
Compound: 10b
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs under normoxic condition by MTT assay
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs under normoxic condition by MTT assay
[PMID: 31972394]
MDA-MB-468 IC50
3.03 μM
Compound: 10b
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs under CoCl2-induced hypoxic condition by MTT assay
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs under CoCl2-induced hypoxic condition by MTT assay
[PMID: 31972394]
In Vitro

CDK2-IN-12 (compound 10b) exerts outstanding anti-proliferative activity against leukemia (CCRF-CEM, HL-60TB, K-562 and MOLT-4), non-small cell lung cancer (HOP-92), colon cancer (COLO 205, HCT-116 and SW-620), renal (ACHN) and breast (MDA-MB-468) cell lines with GI% (percentage growth inhibition) ranging from 80 to 100%[1].
CDK2-IN-12 displays much enhanced growth inhibitory activity, under normoxic and hypoxic conditions, against MDA-MB-468 (IC50 = 1.37 ± 0.07 and 3.03 ± 0.11 μM) than MCF-7 cells (IC50 = 6.80 ± 0.17 and 15.10 ± 0.82 μM)[1].

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

Molecular Weight

447.47

Formula

C20H17N9O2S

CAS No.
SMILES

O=S(C1=CC=C(/N=N/C2=C3N=C(C4=CC=C(C)C=C4)C(C#N)=C(N)N3N=C2N)C=C1)(N)=O

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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.

Purity & Documentation
References
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CDK2-IN-12
Cat. No.:
HY-150573
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