| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CDK7 0.13 nM (IC50) 166v VP22-GFP 0.02 μM (EC50) 01-6332 0.27 μM (EC50) HIV-1 (NL4.3 strain) 1.04 μM (EC50) 4LIG7 1.13 μM (EC50)
LDC4297 hydrochloride targets cyclin-dependent kinase 7 (CDK7), a serine/threonine kinase that plays a key role in cell cycle regulation and transcription. CDK7 is a component of the CDK-activating kinase (CAK) complex and is essential for the activation of other CDKs involved in cell cycle progression. By potently inhibiting CDK7 with an IC50 of 0.13 nM, LDC4297 hydrochloride disrupts cell cycle progression and transcription, leading to antiviral and antiproliferative effects. |
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| ln Vitro |
LDC4297 hydrochloride (0-10 μM; 6 d) dose-dependently suppresses HCMV replication with an EC50 value of 24.5 nM[1]. LDC4297 hydrochloride (0-10 μM; 4 d) has a GI50 value of 4.5 μM and exhibits anti-proliferative activity against primary cultures of human fibroblasts (HFF)[1]. Via a complex mechanism of action that includes interfering with virus-induced Rb phosphorylation, LDC4297 hydrochloride (20 μM; 12-96 h) has anti-HCMV activity[1]. Broad antiviral activities against HCMV, GPCMV, MCMV, HVV-6A, HSV-1, HSV-2, VZV, EBV, HAdV-2, Vaccinia virus, HIV-1 (nl4-3), HIV-1 (4LIG7), and Influenza A virus are demonstrated by LDC4297 hydrochloride (0-10 μM; 7 d), with EC50 values of 0.02, 0.05, 0.07, 0.04, 0.02, 0.27, 0.06, 1.21, 0.25, 0.77, 1.04, 1.13, and 0.99 μM, respectively[1].
In vitro, LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with an EC50 of 24.5 nM. It shows broad antiviral activities against Herpesviridae, Adenoviridae, Poxviridae, Retroviridae, and Orthomyxoviridae with EC50 values of 0.02-1.21 μM. LDC4297 hydrochloride (0-10 μM; 4 days) has a GI50 value of 4.5 μM and exhibits anti-proliferative activity against primary cultures of human fibroblasts (HFF). |
| ln Vivo |
Pharmacokinetic analyses of LDC4297 hydrochloride (100 mg/kg; po once) are encouraging[1].
In vivo data for LDC4297 hydrochloride is not extensively reported in publicly available sources. As a potent CDK7 inhibitor with broad antiviral activity, the compound has potential applications in animal models of viral infections, including HCMV, herpesviruses, and other viral pathogens. By targeting a host factor essential for viral replication, LDC4297 hydrochloride could provide a broad-spectrum antiviral approach. However, specific published in vivo efficacy studies are not detailed in the current literature. |
| Enzyme Assay |
The in vitro CDK7 inhibition assay for LDC4297 hydrochloride uses recombinant CDK7 kinase and a peptide substrate. Kinase activity is measured using radioactive or luminescent detection methods, and IC50 values are calculated from dose-response curves. Antiviral assays are performed in virus-infected cells, with viral replication measured by plaque reduction assay, qPCR, or cytopathic effect. EC50 values are calculated from dose-response curves.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Primary cultures of fibroblasts derived from human (HFF) with virus infection Tested Concentrations: 20 μM Incubation Duration: 12, 24, 48 and 96 hrs (hours) Experimental Results: demonstrated inhibitory effect towards viral protein synthesis at the stage of immediate early (IE) gene expression and the drug-mediated reduction of IE1p72 levels partially recovered over time. Exerted an inhibitory effect on human cytomegalovirus (HCMV) induced an up-regulation of protein expression or protein phosphorylation, and decreased Rb expression in the uninfected control cells at 24 h. Cellular assays for LDC4297 hydrochloride are conducted in virus-infected cell lines and primary human fibroblasts. Cells are treated with varying concentrations of LDC4297 hydrochloride. Viral replication is measured by plaque reduction assay, qPCR, or cytopathic effect. Cell viability and proliferation are measured using standard assays such as MTT to determine GI50 values. The compound's effects on CDK7 activity are confirmed by measuring phosphorylation of CDK7 substrates. |
| Animal Protocol |
Animal/Disease Models: CD1 mice[1]
Doses: 100 mg/kg Route of Administration: po (oral gavage); 100 mg/kg once Experimental Results: demonstrated a half-life (t1/2z) of 1.6 h, and the time to a mean peak plasma concentration of 1297.6 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%. In vivo studies for LDC4297 hydrochloride would typically involve animal models of viral infections, such as HCMV or other herpesvirus infections. The compound would be administered via intraperitoneal or oral routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring viral loads in tissues and clinical signs of infection. However, specific published in vivo protocols for LDC4297 hydrochloride are not available in the current literature. The compound is currently used as a research tool. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for LDC4297 hydrochloride is not extensively reported in publicly available sources. The compound has a molecular weight of 468.98 g/mol and a molecular formula of C23H29ClN8O. It has a CAS number of 2319747-14-1. As a small molecule CDK7 inhibitor, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life are not available in the current literature for this research compound.
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| Toxicity/Toxicokinetics |
Toxicity data for LDC4297 hydrochloride is limited in publicly available sources. As with all research compounds, LDC4297 hydrochloride is intended for research use only and not for human therapeutic applications. The compound's potent CDK7 inhibition suggests potential on-target toxicities that would need to be addressed. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
LDC4297 hydrochloride (CAS 2319747-14-1) is a selective CDK7 inhibitor with an IC50 of 0.13 nM. It inhibits HCMV replication (EC50 = 24.5 nM) and shows broad antiviral activity against multiple virus families (EC50 = 0.02-1.21 μM). It has a GI50 of 4.5 μM in human fibroblasts. LDC4297 hydrochloride has a molecular formula of C23H29ClN8O and a molecular weight of 468.98 g/mol. It is a valuable research tool for studying CDK7 biology and antiviral strategies.
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| Molecular Formula |
C23H29CLN8O
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|---|---|
| Molecular Weight |
468.982362508774
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| Exact Mass |
468.215
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| CAS # |
2319747-14-1
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| Related CAS # |
LDC4297;1453834-21-3
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| PubChem CID |
137958370
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
594
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1C=NN2C(=NC(OC3CNCCC3)=NC=12)NCC1C=CC=CC=1N1N=CC=C1)(C)C.Cl
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| InChi Key |
CEUJJAKJRBKKSL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H28N8O.ClH/c1-16(2)19-15-27-31-21(19)28-23(32-18-8-5-10-24-14-18)29-22(31)25-13-17-7-3-4-9-20(17)30-12-6-11-26-30;/h3-4,6-7,9,11-12,15-16,18,24H,5,8,10,13-14H2,1-2H3,(H,25,28,29);1H
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| Chemical Name |
2-piperidin-3-yloxy-8-propan-2-yl-N-[(2-pyrazol-1-ylphenyl)methyl]pyrazolo[1,5-a][1,3,5]triazin-4-amine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (213.23 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1323 mL | 10.6614 mL | 21.3229 mL | |
| 5 mM | 0.4265 mL | 2.1323 mL | 4.2646 mL | |
| 10 mM | 0.2132 mL | 1.0661 mL | 2.1323 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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