75567-37-2
Ingenol-3- angelate
CAS: 75567-37-2
Molecular Formula: C25H34O6
75567-37-2 - Names and Identifiers
75567-37-2 - Physico-chemical Properties
| Molecular Formula | C25H34O6 |
| Molar Mass | 430.53 |
| Density | 1.26±0.1 g/cm3(Predicted) |
| Boling Point | 576.9±50.0 °C(Predicted) |
| Water Solubility | Soluble in 100% ethanol, DMSO, dichloromethane, and methanol. Insoluble in water. |
| Solubility | DMSO : ≥ 100 mg/mL (232.27 mM) |
| Appearance | Powder |
| Color | white to beige |
| pKa | 11.52±0.70(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. |
| MDL | MFCD07784504 |
| Physical and Chemical Properties | White powder, soluble in methanol, ethanol, DMSO and other organic solvents, comes from the whole plant of Euphorbiaceae (Euphorbia). |
| In vitro study | Ingenol Mebutate (Ingenol 3-angelate) is an active ingredient in Euphorbia peplus , acting as a potent PKC activator, with K i s of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively. Ingenol Mebutate also EC 50 s of 13 ± 2.4 nM (PKC-α), 4.37 ± 0.4 nM (PKC-βI), 10.5 ± 2.2 nM (PKC-βII), 38.6 ± 2.9 nM (PKC-δ), 1.08 ± 0.01 nM (PKC-ε), 0.9 ± 0.13 nM (PKC-μ) in WEHI-231 cells, 198 ± 12.5 nM (PKC-α), 69.1 ± 8.2 nM (PKC-βI), 4.6 ± 0.4 nM (PKC-ε) and 1 nM (PKC-μ) in HOP-92 cells, 635 ± 245 nM (PKC-α), 146 ± 35 nM (PKC-βI), 4.7 ± 0.7 nM (PKC-δ), 1.1 ± 0.5 nM (PKC-ε), and 30 nM (PKC-μ) in Colo-205 cells. Ingenol Mebutate sensitizes WEHI-231 cells, HOP-92 and Colo-205 cells, with IC 50 s of 1.41 ± 0.255 nM, 3.24 ± 2.01 nM, and 11.9 ± 1.307 nM, respectively. Ingenol Mebutate (PEP005; 20 nM) actions are PKC-δ dependent, induces apoptosis in primary AML marrow blasts but not in normal myeloblasts. Ingenol Mebutate (PEP005) activates PKCδ and inhibits PKCα. Colo205-R cells (IC 50 : >10 μM) are >300-fold more resistant to Ingenol Mebutate than parental Colo205-S cells. |
75567-37-2 - Reference Information
| Biological activity | Ingenol Mebutate is the active ingredient in Euphorbia peplus and is a regulator of PKC. The Ki values of PKC-α,PKC-β,PKC-γ,PKC-δ and PKC-ε are 0.3,0.105,0.162,0.376 and 0.171 nM respectively. |
| target | PKC-β 0.105 nM (Ki) PKC-γ 0.162 nM (Ki) PKC-ε 0.171 nM (Ki) PKC-α 0.3 nM (Ki) PKC-δ 0.376 nM (Ki) |
| in vitro study | Ingenol Mebutate (Ingenol 3-angelate) is an active ingredient in Euphorbia peplus , acting as a potent PKC activator, with K I s of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively. Ingenol Mebutate also EC 50 s of 13±2.4 nM (PKC-α), 4.37±0.4 nM (PKC-βI), 10.5±2.2 nM (PKC-βII), 38.6±2.9 nM (PKC-δ), 1.08±0.01 nM (PKC-ε), 0.9±0.13 nM (PKC-μ) in WEHI-231 cells, 198±12.5 nM (PKC-α), 69.1±8.2 nM (PKC-βI), 4.6±0.4 nM (PKC-ε) and 1 nM (PKC-μ) in HOP-92 cells, 635±245 nM (PKC-α), 146±35 nM (PKC-βI), 4.7±0.7 nM (PKC-δ), 1.1±0.5 nM (PKC-ε), and 30 nM (PKC-μ) in Colo-205 cells. Ingenol Mebutate sensitizes WEHI-231 cells, HOP-92 and Colo-205 cells, with IC 50 s of 1.41±0.255 nM, 3.24±2.01 nM, and 11.9±1.307 nM, respectively. Ingenol Mebutate (PEP005; 20 nM) actions are PKC-δ dependent, induces apoptosis in primary AML marrow blars but not in normal myeloblasts. Ingenol Mebutate (PEP005) activates PKCδ and inhibits PKCα. Colo205-R cells (IC 50 : >10 μ m) are >300-fold more resistant to Ingenol Mebutate than parental Colo205-S cells. |
| chemical properties | white powder, soluble in methanol, ethanol, DMSO and other organic solvents, derived from the whole plant of Euphorbiaceae (Euphorbia). |
| use | for content determination/identification/pharmacological experiments, etc. |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 21:54:55
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