(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide WP 1066
WP1066
CAS: 857064-38-1
Molecular Formula: C17H14BrN3O
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide WP 1066 - Names and Identifiers
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide WP 1066 - Physico-chemical Properties
| Molecular Formula | C17H14BrN3O |
| Molar Mass | 356.22 |
| Density | 1.425 |
| Melting Point | 90-93oC |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
| Appearance | Off-white solid |
| Color | White |
| Storage Condition | +2C to +8C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| In vitro study | WP1066 significantly inhibited the growth of HEL cells carrying the JAK2 V617F mutant subtype in a dose-dependent manner with IC20, IC50 and IC80 of 0.8, 2.3 and 3.8 μm, respectively. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μm can inhibit JAK2, STAT3, phosphorylation of STAT5 and ERK1/2, but does not inhibit the phosphorylation of JAK1 and jak3. Concentrations of WP1066 between 0.5 and 3.0 μm inhibited proliferation of AML-like cells obtained from patients as well as AML cell lines OCIM2 and K562 in a dose-dependent manner. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μm decreased JAK2 and pJAK2 protein levels in both OCIM2 and K562 cells in a dose-dependent manner, while STAT3, phosphorylation levels of STAT5 and AKT. WP1066 at a concentration of 2 μm can inhibit the increase of OCIM2 cells by inducing the accumulation of cells in the G0-G1 phase of the cell cycle. 1, 2 or 3 μm of WP1066 can activate procaspase-3, split PARP, and induce apoptosis of OCIM2 and K562 cells in a dose-dependent manner. 5 μm concentration of WP1066 can prevent STAT3 phosphorylation, and 2.5 μm concentration can significantly inhibit the survival and proliferation of Caki-1 and 786-O renal cell carcinoma cells. 5 M WP1066 can also inhibit the expression of HIF1α and HIF2α and the production of VEGF in Caki-1 and 786-O renal cell carcinoma cells. |
| In vivo study | Oral administration of WP1066 at a dose of 40 mg/kg daily for 19 days significantly inhibited tumor growth in Caki-1 of transplanted mice, while decreased phosphorylated STAT3 immunostaining and reduced CD34 positive vessel length. |
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide WP 1066 - Risk and Safety
| HS Code | 29333990 |
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide WP 1066 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.807 ml | 14.036 ml | 28.073 ml |
| 5 mM | 0.561 ml | 2.807 ml | 5.615 ml |
| 10 mM | 0.281 ml | 1.404 ml | 2.807 ml |
| 5 mM | 0.056 ml | 0.281 ml | 0.561 ml |
Last Update：2024-01-02 23:10:35
(2E)-3-(6-Bromo-2-pyridinyl)-2-cyano-N-[(1S)-1-phenylethyl]-2-propenamide WP 1066 - Reference Information
| Use | (2E)-3-(6-bromo-2-pyridyl)-2-cyano-n-[(1S)-1-phenylethyl]-2-acrylamide is a compound useful in the treatment of cell proliferative diseases such as cancer. The present compounds have significant potency as kinase inhibitors, down-regulating by c-myc and inhibiting the growth and survival of cancer cell lines. |
| biological activity | WP1066 is a novel JAK2 and STAT3 inhibitor, in HEL cells, the IC50 was 2.30 μm and 2.43 μm, respectively; It had inhibitory activity on JAK2,STAT3,STAT5 and ERK1/2, but had no effect on JAK1 and jak3. WP1066 can induce apoptosis. Phase 1. |
| Target | TargetValue JAK2 (HEL cells) 2.3 μm STAT3 (HEL cells) 2.43 μm |
| Target | Value |
| JAK2 (HEL cells) | 2.3 μM |
| STAT3 (HEL cells) | 2.43 μM |
| in vitro study | WP1066 can significantly inhibit the growth of HEL cells carrying JAK2 V617F mutant subtype, this inhibition was dose-dependent with IC20, IC50 and IC80 of 0.8, 2.3 and 3.8 μm, respectively. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μm can inhibit JAK2, STAT3, phosphorylation of STAT5 and ERK1/2, but does not inhibit the phosphorylation of JAK1 and jak3. Concentrations of WP1066 between 0.5 and 3.0 μm inhibited proliferation of AML-like cells obtained from patients as well as AML cell lines OCIM2 and K562 in a dose-dependent manner. WP1066 at concentrations of 0.5, 1.0, 2.0, 3.0, or 4.0 μm decreased JAK2 and pJAK2 protein levels in both OCIM2 and K562 cells in a dose-dependent manner, while STAT3, phosphorylation levels of STAT5 and AKT. WP1066 at a concentration of 2 μm can inhibit the increase of OCIM2 cells by inducing the accumulation of cells in the G0-G1 phase of the cell cycle. 1, 2 or 3 μm of WP1066 can activate procaspase-3, split PARP, and induce apoptosis of OCIM2 and K562 cells in a dose-dependent manner. 5 μm concentration of WP1066 can prevent STAT3 phosphorylation, and 2.5 μm concentration can significantly inhibit the survival and proliferation of Caki-1 and 786-O renal cell carcinoma cells. 5 M WP1066 can also inhibit the expression of HIF1α and HIF2α and the production of VEGF in Caki-1 and 786-O renal cell carcinoma cells. |
| in vivo study | WP1066 was administered orally at a dose of 40 mg/kg daily for 19 consecutive days, it can significantly inhibit the tumor growth of Caki-1 transplanted mice, and at the same time, the phosphorylation of STAT3 immunostaining decreased, and the length of CD34 positive vessels decreased. |
Last Update：2024-04-09 21:54:55
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Spot supply
Product Name: WP1066 Visit Supplier Webpage Request for quotationCAS: 857064-38-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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