ChemicalBook > CAS DataBase List > LDC4297

LDC4297

Product Name: LDC4297
CAS No.: 1453834-21-3
Chemical Name: LDC4297
Synonyms: LDC4297;CS-2540;CS-2539;LDC044297;LDC4297;LDC 4297;LDC4297(LDC044297);LDC4297 (LDC044297) ，S7992;N-(2-(1H-Pyrazol-1-yl)benzyl)-8-isopropyl-2-(piperidin-3-yloxy)pyrazolo[1,5-a][1,3,5]triazin-4-amine;Pyrazolo[1,5-a]-1,3,5-triazin-4-amine, 8-(1-methylethyl)-2-(3-piperidinyloxy)-N-[[2-(1H-pyrazol-1-yl)phenyl]methyl]-
CBNumber: CB53171481
Molecular Formula: C23H28N8O
Formula Weight: 432.52
MOL File: 1453834-21-3.mol

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LDC4297 Property

Density: 1.37±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMF:20.0(Max Conc. mg/mL);46.24(Max Conc. mM)
DMSO:40.0(Max Conc. mg/mL);92.48(Max Conc. mM)
Ethanol:20.0(Max Conc. mg/mL);46.24(Max Conc. mM)
form: A crystalline solid
pka: 8.69±0.10(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23398
Product name: LDC-4297
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 23398
Product name: LDC-4297
Purity: ≥98%
Packaging: 5mg
Price: $161
Updated: 2024/03/01

Cayman Chemical

Product number: 23398
Product name: LDC-4297
Purity: ≥98%
Packaging: 10mg
Price: $283
Updated: 2024/03/01

Cayman Chemical

Product number: 23398
Product name: LDC-4297
Purity: ≥98%
Packaging: 25mg
Price: $573
Updated: 2024/03/01

TRC

Product number: L367665
Product name: LDC4297
Packaging: 25mg
Price: $3795
Updated: 2021/12/16

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LDC4297 Chemical Properties,Usage,Production

Description

LDC-4297 is an inhibitor of cyclin-dependent kinase 7 (CDK7; IC₅₀ = <5 nM). It is selective for CDK7 over CDK4, CDK6, and CDK9 (IC₅₀s = >10, >10, and 1.71 μM), however, it also inhibits CDK2 and CDK1 (IC₅₀s = 6.4 and 53.7 nM, respectively). LDC-4297 (10-100 nM) induces apoptosis in A549, HeLa, and HCT116 cancer cells in a concentration-dependent manner. It inhibits human cytomegalovirus (HCMV) replication in human fibroblasts (EC₅₀ = 24.5 nM). LDC-4297 also reduces replication of Herpesviridae, Adenoviridae, Poxviridae, Retroviridae, and Orthomyxoviridae family viruses (EC₅₀s = 0.02-1.13 μM).

Uses

Cyclin-dependent protein kinase 7 (CDK7) is involved with a broad range of regulatory roles in cell cycle and transcription, which is essential for viral replication. LDC 4297 is a CDK7 inhibitor that can be used to develop antiviral drugs.

Definition

ChEBI: LDC4297 is a pyrazolotriazine that is pyrazolo[1,5-a][1,3,5]triazine substituted by a piperidin-3-yloxy group, [2-(1H-pyrazol-1-yl)benzyl]nitrilo group and an isopropyl group at positions 2, 4 and 8 respectively. It is a potent and selective CDK7 inhibitor and exhibits antiviral activity. It has a role as an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor, an apoptosis inducer, an antineoplastic agent and an antiviral agent. It is a pyrazolotriazine, a member of pyrazoles, a member of piperidines, a secondary amino compound and an aromatic ether.

in vivo

LDC4297 (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses^[1].

Animal Model:	CD1 mice^[1]
Dosage:	100 mg/kg
Administration:	Oral gavage; 100 mg/kg once
Result:	Showed a half-life of 1.6 h, and the time to a mean peak plasma concentration of 1,297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%.

IC 50

CDK7: 0.13 nM (IC₅₀); HSV-1: 0.02 μM (EC₅₀); HSV-2: 0.27 μM (EC₅₀)

References

[1] TIMOTHY W R KELSO. Cyclin-dependent kinase 7 controls mRNA synthesis by affecting stability of preinitiation complexes, leading to altered gene expression, cell cycle progression, and survival of tumor cells.[J]. Molecular and Cellular Biology, 2014, 34 19: 3675-3688. DOI: 10.1128/mcb.00595-14
[2] CORINA HUTTERER. A novel CDK7 inhibitor of the Pyrazolotriazine class exerts broad-spectrum antiviral activity at nanomolar concentrations.[J]. Antimicrobial Agents and Chemotherapy, 2015, 59 4: 2062-2071. DOI: 10.1128/aac.04534-14

LDC4297 Preparation Products And Raw materials

Raw materials

Preparation Products

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1453834-21-3, LDC4297Related Search:

LDC4297

LDC4297(LDC044297)

LDC044297

LDC4297;LDC 4297

CS-2539

CS-2540

Pyrazolo[1,5-a]-1,3,5-triazin-4-amine, 8-(1-methylethyl)-2-(3-piperidinyloxy)-N-[[2-(1H-pyrazol-1-yl)phenyl]methyl]-

N-(2-(1H-Pyrazol-1-yl)benzyl)-8-isopropyl-2-(piperidin-3-yloxy)pyrazolo[1,5-a][1,3,5]triazin-4-amine

LDC4297 (LDC044297) ，S7992

1453834-21-3