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CDDO-2P-Im

Alias: CDDO2PIm; CDDO 2P Im
Cat No.:V39613 Purity: ≥98%
CDDO-2P-Im is an imidazolamide analog of CDDO with chemopreventive effects.
CDDO-2P-Im
CDDO-2P-Im Chemical Structure CAS No.: 1883650-96-1
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
CDDO-2P-Im is an imidazolamide analog of CDDO with chemopreventive effects. CDDO-2P-Im reduces the size and severity of lung tumors in a mouse lung cancer model.
CDDO-2P-Im (CAS 1883650-96-1) is an imidazolamide analog of CDDO with chemopreventive effects. This compound demonstrates potential in reducing tumor size and severity in mouse models of lung cancer. CDDO-2P-Im significantly elevates heme oxygenase-1 (HO-1) and quinone reductase (NQO1) mRNA and protein levels in various mouse tissues.
Biological Activity I Assay Protocols (From Reference)
Targets
Others (chemopreventive targets including NQO1 and HO-1). CDDO-2P-Im acts through the induction of phase 2 detoxifying enzymes such as quinone reductase (NQO1) and heme oxygenase-1 (HO-1), contributing to its chemopreventive effects.
ln Vitro
At 100 nM, CDDO-2P-Im (100 nM; 4 days) stimulates U937 cell differentiation [1]. With an IC50 of 5.8 nM, CDDO-2P-Im suppresses the generation of NO in RAW264.7 cells[1].
At 100 nM, CDDO-2P-Im stimulates U937 cell differentiation over 4 days. The compound suppresses the generation of nitric oxide (NO) in RAW264.7 cells with an IC50 of 5.8 nM. These activities demonstrate its immunomodulatory and anti-inflammatory properties.
ln Vivo
Compared to CDDO-Im, CDDO-2P-Im was more stable in pharmacokinetic investigations [1]. In a variety of mouse tissues in vivo, CDDO-2P-Im dramatically raises the levels of quinone reductase (NQO1) and heme oxygenase-1 (HO-1) mRNA and protein [1]. In A/J mice, CDDO-2P-Im (50–200 mg/kg; diet; 16 weeks) decreases the quantity, size, and severity of tumors [1].
In A/J mice, CDDO-2P-Im (50–200 mg/kg administered via diet for 16 weeks) decreases the number, size, and severity of tumors. The compound dramatically elevates HO-1 and NQO1 mRNA and protein levels in various mouse tissues. CDDO-2P-Im is more stable than CDDO-Im in pharmacokinetic studies.
Enzyme Assay
Cell-based assays are conducted using U937 cells treated with CDDO-2P-Im at concentrations of 30 nM and 100 nM for 4 days to assess differentiation. In RAW264.7 cells, the compound's ability to suppress NO production is evaluated, with an IC50 of 5.8 nM determined.
Cell Assay
Apoptosis analysis [1]
Cell Types: U937 Cell
Tested Concentrations: 30 nM, 100 nM
Incubation Duration: 4 days
Experimental Results: 100 nM induced U937 cell differentiation.
In vitro studies use U937 cells to evaluate differentiation at 30–100 nM over 4 days. RAW264.7 macrophages are used to assess the inhibition of NO production, providing insight into the compound's anti-inflammatory mechanism.
Animal Protocol
Animal/Disease Models: Sevenweeks old female A/J mice [1]
Doses: 50 mg/kg, 200 mg/kg
Route of Administration: diet; continued for 16 weeks
Experimental Results: The number, size and severity of tumors were diminished.
In vivo studies are performed in seven-week-old female A/J mice. CDDO-2P-Im is administered via diet at doses of 50 mg/kg and 200 mg/kg for 16 weeks. Tumor number, size, and severity are evaluated, along with the measurement of HO-1 and NQO1 levels in tissues.
ADME/Pharmacokinetics
CDDO-2P-Im demonstrates improved stability compared to CDDO-Im in pharmacokinetic investigations. The compound's enhanced PK profile supports its in vivo efficacy. Detailed PK parameters would require further investigation from primary literature sources.
Toxicity/Toxicokinetics
Comprehensive toxicity data for CDDO-2P-Im are not extensively reported in the available literature. The compound is intended for research use only. Its chemopreventive effects and induction of cytoprotective enzymes suggest a favorable safety profile.
References
[1]. Cao M , et al. Novel synthetic pyridyl analogues of CDDO-Imidazolide are useful new tools in cancer prevention. Pharmacol Res. 2015 Oct;100:135-47.
Additional Infomation
CDDO-2P-Im is a research compound used in cancer chemoprevention studies. It is a synthetic triterpenoid analogue with potential applications in preventing lung cancer. The compound is not approved for clinical use and is supplied for research purposes only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C39H46N4O3
Molecular Weight
618.807549953461
Exact Mass
618.356
CAS #
1883650-96-1
PubChem CID
135397767
Appearance
Typically exists as solid at room temperature
LogP
7.1
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
2
Heavy Atom Count
46
Complexity
1480
Defined Atom Stereocenter Count
7
SMILES
C[C@@]12CC[C@]3(CCC(C[C@H]3[C@H]1C(=O)C=C4[C@]2(CC[C@@H]5[C@@]4(C=C(C(=O)C5(C)C)C#N)C)C)(C)C)C(=O)N6C=C(N=C6)C7=CC=CC=N7
InChi Key
NXUDOCUNEVFUGK-DIJMLVISSA-N
InChi Code
InChI=1S/C39H46N4O3/c1-34(2)13-15-39(33(46)43-22-27(42-23-43)26-10-8-9-17-41-26)16-14-38(7)31(25(39)20-34)28(44)18-30-36(5)19-24(21-40)32(45)35(3,4)29(36)11-12-37(30,38)6/h8-10,17-19,22-23,25,29,31H,11-16,20H2,1-7H3/t25-,29-,31-,36-,37+,38+,39-/m0/s1
Chemical Name
(4aR,6aR,6aS,6bR,8aS,12aS,14bS)-4,4,6a,6b,11,11,14b-heptamethyl-3,13-dioxo-8a-(4-pyridin-2-ylimidazole-1-carbonyl)-4a,5,6,6a,7,8,9,10,12,12a-decahydropicene-2-carbonitrile
Synonyms
CDDO2PIm; CDDO 2P Im
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~200 mg/mL (~323.20 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6160 mL 8.0800 mL 16.1600 mL
5 mM 0.3232 mL 1.6160 mL 3.2320 mL
10 mM 0.1616 mL 0.8080 mL 1.6160 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.

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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.
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