| Identification | Back Directory | [Name]
N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide Hcl | [CAS]
902135-91-5 | [Synonyms]
CS-266
AT 7519
AT7519 HCl
AT-7519(HCI)
AT7519; AT-7519
AT7519 HCl, >=99%
AT 7519 HCl salt
Light yellow solid
AT7519 (Hydrochloride)
AT 7519 hydrochloride salt
AT7519;AT-7519;AT 7519 HYDROCHLORIDE;AT-7519 HYDROCHLORIDE
4-(2,6-Dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide HCl
N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide Hcl
4-(2,6-Dichlorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide hydrochloride
N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide hydrochloride
4-(2,6-Dichlorobenzoylamino)-1H-pyrazole-3-carboxylic Acid Piperidin-4-ylamide Monohydrochloride
AT 7519
N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide hydrochloride | [Molecular Formula]
C16H18Cl3N5O2 | [MDL Number]
MFCD14636428 | [MOL File]
902135-91-5.mol | [Molecular Weight]
418.7 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
≥29.93 mg/mL in H2O; ≥43.3 mg/mL in DMSO with ultrasonic; ≥8.82 mg/mL in EtOH with ultrasonic | [form ]
crystalline solid | [color ]
White to off-white | [InChI]
InChI=1S/C16H17Cl2N5O2.ClH/c17-10-2-1-3-11(18)13(10)15(24)22-12-8-20-23-14(12)16(25)21-9-4-6-19-7-5-9;/h1-3,8-9,19H,4-7H2,(H,20,23)(H,21,25)(H,22,24);1H | [InChIKey]
PAOFPNGYBWGKCO-UHFFFAOYSA-N | [SMILES]
N(C1=CNN=C1C(=O)NC1CCNCC1)C(C1C(=CC=CC=1Cl)Cl)=O.Cl |
| Hazard Information | Back Directory | [Description]
AT7519 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) with IC50 values of 210, 47, 100, 13, 170, and <10 nM for Cdk1, 2, 4, 5, 6, and 9, respectively.1 It is less potent against Cdk3 and Cdk7 and inactive against non-Cdk kinases save for GSK3β (IC50 = 89 nM).1 AT7519 demonstrates antiproliferative activity against a wide variety of human tumor cell lines (IC50s = 40-940 nM in vitro), inhibiting cell cycle progression and inducing apoptosis, and prevents tumor growth in human tumor xenograft models.1,2 AT7519 induces activation of GSK3β by down-regulating GSK3β phosphorylation, which contributes to AT7519-induced apoptosis.2 | [Uses]
4-(2,6-DichlorobenzoylaMino)-1H-pyrazole-3-carboxylic Acid Piperidin-4-ylaMide Monohydrochloride is used in the structure based design of a cyclin-dependant kinase CDK2 inhibitor.
| [in vivo]
AT7519 inhibits tumor growth in a human MM xenograft mouse model[1]. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice[2]. | [IC 50]
CDK9/Cyclin T: 10 nM (IC50); CDK5/p35: 13 nM (IC50); cdk2/cyclin A: 47 nM (IC50); Cdk4/cyclin D1: 100 nM (IC50); cdk6/cyclin D3: 170 nM (IC50); Cdk1/cyclin B: 210 nM (IC50); CDK7/Cyclin H/MAT1: 2400 nM (IC50); GSK3β: 89 nM (IC50) | [References]
[1] MATTHEW S SQUIRES. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines.[J]. Molecular Cancer Therapeutics, 2009, 8 2: 324-332. DOI: 10.1158/1535-7163.mct-08-0890
[2] L SANTO. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3β activation and RNA polymerase II inhibition[J]. Oncogene, 2010, 29 16: 2325-2336. DOI: 10.1038/onc.2009.510 |
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