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CAY10574

Names

[ CAS No. ]:
140651-18-9

[ Name ]:
CAY10574

[Synonym ]:
3tn8
2clx
Cdk9 Inhibitor II
Phenol, 4-[(E)-2-(3,5-diamino-1H-pyrazol-4-yl)diazenyl]-
4-[(E)-(3,5-Diamino-1H-pyrazol-4-yl)diazenyl]phenol
F18
CAN-508

Biological Activity

[Description]:

CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

[Target]

CDK9/cyclinT1:0.35 μM (IC50)

CDK2/cyclinE:20 μM (IC50)

cdk2/cyclin A:69 μM (IC50)

Cdk4/cyclin D1:13.5 μM (IC50)

CDK7/cyclin H:26 μM (IC50)

Cdk1/cyclin B:44 μM (IC50)


[In Vitro]

CAN508 reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays[1]. CAN508 (20-40 μM; 72 hours) significantly reduces cell proliferation in a dose dependent manner in all three esophageal adenocarcinoma cell lines (SKGT4, OE33 and FLO-1 cells) with IC50s ranging from 34.99 to 91.09 μM[2]. CAN508 (40 μM; 72 hours) increases apoptosis in all three esophageal adenocarcinoma cells[2]. Apoptosis Analysis[1] Cell Line: SKGT4, OE33 and FLO-1 cells Concentration: 40 μM Incubation Time: 72 hours Result: Increased apoptosis by 2 fold in all three esophageal adenocarcinoma cells compared to untreated controls.

[In Vivo]

CAN508 (60 mg/kg; i.p.; daily for 10 days) has antitumor effects in esophageal adenocarcinoma xenografts[1]. Animal Model: 4 weeks-old female nude mice (esophageal adenocarcinoma xenografts)[1] Dosage: 60 mg/kg Administration: I.p.; daily for 10 days Result: Caused reduction of tumor growth starting from post-treatment day three with 50.83% reduction.

[References]

[1]. Krystof V, et al. 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006;49(22):6500-6509.

[2]. Tong Z, et al. Antitumor effects of cyclin dependent kinase 9 inhibition in esophageal adenocarcinoma. Oncotarget. 2017;8(17):28696-28710.

Chemical & Physical Properties

[ Density]:
1.7±0.1 g/cm3

[ Boiling Point ]:
638.3±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C9H10N6O

[ Molecular Weight ]:
218.215

[ Flash Point ]:
339.8±31.5 °C

[ Exact Mass ]:
218.091614

[ PSA ]:
125.67000

[ LogP ]:
0.40

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.803

Related Compounds