1. Cell Cycle/DNA Damage
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  3. CDK5 inhibitor 20-223

CDK5 inhibitor 20-223 

目录号: HY-123772 纯度: 99.64%
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CDK5 inhibitor 20-223 是一种有效的 CDK2CDK5 抑制剂,IC50 分别为 6.0 和 8.8 nM。CDK5 inhibitor 20-223 有潜力用于结肠直肠癌 (CRC) 的研究。

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CDK5 inhibitor 20-223 Chemical Structure

CDK5 inhibitor 20-223 Chemical Structure

CAS No. : 865317-30-2

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Description

CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent[1].

IC50 & Target[1]

CDK2

6.0 nM (IC50)

CDK5

8.8 nM (IC50)

In Vitro

CDK5 inhibitor 20-223 (10 nM-10 μM; 72 hours) potently inhibits cell growth in a panel of colorectal cancer (CRC) cell lines[1].
CDK5 inhibitor 20-223 (0.3125-20 μM; 6 hours) induces a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels in each of the three CRC cell lines[1].

Cell Viability Assay[1]

Cell Line: CRC cell lines SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells
Concentration: 10 μM, 1 μM, 100 nM, 10 nM
Incubation Time: 72 hours
Result: Reduced cell growth. IC50s of 168±20, 480±41, 360±72, 763±92, 117±49, 568±49, 79±31 nM for SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells.

Western Blot Analysis[1]

Cell Line: CRC cell lines GEO, HCT116 and HT29
Concentration: 20, 10, 5, 2.5, 1.25, 0.625, 0.3125 μM
Incubation Time: 6 hours
Result: Did not affect the total levels of CDK2/5, and the levels of total FAK or total Retinoblastoma protein (Rb).
Induced a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels.
In Vivo

CDK5 inhibitor 20-223 (8mg/kg; subcutaneously; for 14 injections) shows anti-tumor activity in human CRC xenograft tumors in nude mice[1].

Animal Model: Athymic nude mice[1]
Dosage: 8 mg/kg
Administration: Injections were given subcutaneously daily for the first week and every other day for two more weeks for a total of 14 injections.
Result: Reduced tumor growth and tumor weight in vivo.
Molecular Weight

305.37

Formula

C₁₉H₁₉N₃O

CAS No.

865317-30-2

SMILES

O=C(NC1=NNC(C2CCC2)=C1)CC3=CC=C4C=CC=CC4=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

CDK5 inhibitor 20-223CDKCyclin dependent kinaseCDK2CDK5colorectalcancerCRCInhibitorinhibitorinhibit

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产品名称:
CDK5 inhibitor 20-223
目录号:
HY-123772
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