CDDO-Im free base · Synonyms: RTA-403 | TP-235
CDDO-Im is an activator of Nrf2.
For research use only. Not for human or veterinary use.
CDDO-Im structure
CAS No.: 443104-02-7
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 500 mg | USD 580.00 | BP-02071-500mg | In stock | Get quote |
| 1 g | USD 880.00 | BP-02071-1g | In stock | Get quote |
| 5 g | Inquire | BP-02071-5g | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
Description
CDDO-Im (RTA-403) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ.
Biological activity
In Vitro CDDO-Im is highly active in suppressing cellular proliferation of human leukemia and breast cancer cell lines (IC50 approximately 10-30 nM). In U937 leukemia cells, CDDO-Im also induces monocytic differentiation as measured by increased cell surface expression of CD11b and CD36. Treatment with CDDO-Im elevates protein levels of Nrf2, a transcription factor previously shown to bind ARE sequences, and increases expression of a number of antioxidant and detoxification genes regulated by Nrf2. CDDO-Im is one of the most potent synthetic triterpenoids shown to induce growth inhibition and apoptosis in various human cancer cells, including multiple myeloma, lung, pancreas and breast cancer. CDDO-Im treatment markedly induces cell cycle arrest at G2/M-phase and apoptosis in the triple-negative breast cancer cell lines, SUM159 and MDA-MB-231. The CD24 /EpCAM+ cells in SUM159 tumorspheres are significantly inhibited by CDDO-Im treatment. CDDO-Im also significantly decreases sphere forming efficiency and tumorsphere size in both primary and secondary sphere cultures. In Vivo CDDO-Im is a potent inhibitor of de novo inducible nitric oxide synthase expression in primary mouse macrophages. Moreover, CDDO-Im inhibits growth of B16 murine melanoma and L1210 murine leukemia cells in vivo. Injection of 10 nM (5.4 μg) of CDDO-Im almost completely blocks the ability of IFN-γ to induce iNOS, and treatment with as little as 1 nmol of CDDO-Im (0.54 μg) is partially effective.
Identifiers
- SMILES
-
[H][C@@]12CC(C)(C)CC[C@@]1(CC[C@]1(C)[C@]2([H])C(=O)C=C2[C@@]1(C)CC[C@@]1([H])C(C)(C)C(=O)C(=C[C@]21C)C#N)C(=O)N1C=CN=C1 - InChIKey
-
ITFBYYCNYVFPKD-FMIDTUQUSA-N
Specifications
- MW (average)
- 541.7235
- Formula
- C34H43N3O3
- CAS No.
- 443104-02-7
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO