| 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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| 250mg | |||
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| Targets |
CG347B targets histone deacetylase 6 (HDAC6). HDAC6 is a class IIb histone deacetylase that deacetylates non-histone proteins, including α-tubulin and Hsp90, and is involved in the regulation of protein acetylation and cellular processes. By selectively inhibiting HDAC6, CG347B modulates acetylation of its substrates, which has implications for oncology, immunology, and neurology research.
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| ln Vitro |
HtrA1 was shown to be a gene related with cisplatin (CDDP) resistance in NSCLC cells, and in CDDP-resistant NCI-H460 cells, CG347B had no influence on HtrA1's normalized mRNA expression or protein levels [1]. The study found that CG347B (200 nM; 48 h) somewhat alleviated the inhibition of Foxp3 expression generated by IL-4 (15 ng/mL) and demonstrated histone deacetylation in naive CD4+ T cells from WT B6 mice that were grown under Treg polarizing conditions. (1-3 d) is when potential inhibition happens [3].
CG347B demonstrates selective inhibition of HDAC6 in vitro. Its selectivity for HDAC6 over other HDAC isoforms has been characterized in enzymatic assays. The compound's activity is assessed by measuring HDAC6 enzyme activity using fluorogenic substrates. Its IC50 for HDAC6 inhibition and selectivity profile are key parameters. Detailed quantitative data are available from the manufacturer. |
| ln Vivo |
CG347B has been studied in vivo for its effects on HDAC6-mediated pathways. As a selective HDAC6 inhibitor, it modulates protein acetylation and cellular processes involved in oncology, immunology, and neurology. Its efficacy in these areas has been evaluated in preclinical models. Detailed in vivo efficacy data are limited in publicly available sources.
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| Enzyme Assay |
HDAC6 enzyme inhibition assays are performed using recombinant human HDAC6 enzyme and a fluorogenic substrate (e.g., acetylated lysine-AMC). The enzyme is incubated with the substrate in assay buffer. Deacetylation allows cleavage of the AMC group by trypsin, generating a fluorescent signal measured at excitation 360 nm, emission 460 nm. CG347B is serially diluted and added to the reaction mixture. IC50 values are determined by non-linear regression analysis. Selectivity assays are performed using other HDAC isoforms (HDAC1, HDAC2, HDAC3, HDAC8, etc.).
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| Cell Assay |
Cellular HDAC6 inhibition is evaluated in cancer cell lines or other relevant cell types. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with CG347B at various concentrations (0.1-10 µM) for 24-72 hours. HDAC6 activity in cell lysates is measured using fluorogenic substrates. Acetylation of HDAC6 substrates (α-tubulin, Hsp90) is measured by Western blotting using anti-acetyl-lysine antibodies. Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays. Each experiment includes known HDAC inhibitors as positive controls.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse models of cancer, immune disorders, or neurological diseases. CG347B is administered orally or intraperitoneally at doses determined by preclinical studies. Disease progression is monitored by clinical scores, tumor growth, or behavioral assessments. Tissue samples are collected for histopathological analysis and biochemical assays (HDAC6 activity, protein acetylation). Sample sizes typically range from 6-10 animals per group. Detailed protocols are available in the literature.
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| ADME/Pharmacokinetics |
CG347B has a molecular weight of 283.33 g/mol and a molecular formula of C16H17N3O2. Chemical name: 2-(1-phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid ethyl ester. Purity: typically 98.1%. Solubility: DMSO. Storage: typically at -20°C. Bioavailability, half-life, and tissue distribution data are not publicly available.
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| Toxicity/Toxicokinetics |
Limited toxicology data are available for CG347B. As an HDAC6 inhibitor, potential toxicities may include effects on protein acetylation in normal tissues. Standard toxicology studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on the immune system and nervous system. No clinical trials have been reported for this compound.
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| References | |
| Additional Infomation |
CG347B is also known as 2-(1-phenyl-cyclopropylamino)-pyrimidine-5-carboxylic acid ethyl ester. It is a selective HDAC6 inhibitor used in oncology, immunology, and neurology research. It can be used as an intermediate in the synthesis of metalloenzyme inhibitors. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
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| Molecular Formula |
C16H17N3O2
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|---|---|
| Molecular Weight |
283.331
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| Exact Mass |
283.132
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| CAS # |
1598426-03-9
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| PubChem CID |
118000986
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
457.2±47.0 °C at 760 mmHg
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| Flash Point |
230.3±29.3 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.641
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| LogP |
2.71
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
357
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC(=O)C1=CN=C(N=C1)NC2(CC2)C3=CC=CC=C3
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| InChi Key |
CTTSUGRYXUPYIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H17N3O2/c1-2-21-14(20)12-10-17-15(18-11-12)19-16(8-9-16)13-6-4-3-5-7-13/h3-7,10-11H,2,8-9H2,1H3,(H,17,18,19)
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| Chemical Name |
ethyl 2-[(1-phenylcyclopropyl)amino]pyrimidine-5-carboxylate
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| Synonyms |
CG 347B; CG-347B; CG347B
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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 |
| 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 : ~250 mg/mL (~882.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (22.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5295 mL | 17.6473 mL | 35.2945 mL | |
| 5 mM | 0.7059 mL | 3.5295 mL | 7.0589 mL | |
| 10 mM | 0.3529 mL | 1.7647 mL | 3.5295 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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