JAK3 Inhibitor
WHI-P154
CAS: 211555-04-3
Molecular Formula: C16H14BrN3O3
JAK3 Inhibitor - Names and Identifiers
| Name | WHI-P154 |
| Synonyms | CS-1516 WHI-P154 JAK3 Inhibitor 2-Bromo-4-((6,7-dimethoxyquinazolin-4-yl)amino)phenol 2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol Phenol, 2-bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]- 4-(3'-Bromo-4'-hydroxyphenyl)amino-6,7-dimethoxyquinazoline WHI-P 154 |
| CAS | 211555-04-3 |
| EINECS | 809-014-9 |
| InChIKey | CBIAKDAYHRWZCU-UHFFFAOYSA-N |
JAK3 Inhibitor - Physico-chemical Properties
| Molecular Formula | C16H14BrN3O3 |
| Molar Mass | 376.2 |
| Density | 1.576±0.06 g/cm3(Predicted) |
| Melting Point | 230 °C |
| Boling Point | 470.3±45.0 °C(Predicted) |
| Solubility | Soluble in DMSO (100 mM). |
| Appearance | powder |
| Color | white to brown |
| pKa | 8.57±0.31(Predicted) |
| Storage Condition | -20°C |
| Use | A JAK3 inhibitor which inhibits other common kinases. |
| In vitro study | WHI-P154 was the first inhibitor to inhibit only JAK3 but not JAK1 and JAK2. WHI-P154 inhibition of STAT1 activation, iNOS expression and NO production in macrophages in vitro. However, studies have shown that WHI-P154 can also inhibit other common kinases including EGFR, Src, Abl, VEGFR, MAPK and PI3-K and induce apoptosis in human glioblastoma cell lines. WHI-P154 inhibits adhesion and migration of malignant glioma cells in the presence of extracellular matrix (ECM). WHI-P154 has obvious cytotoxicity on human malignant glioma cell line U373 and U87, and can induce apoptosis in micro Molar concentration. The anti-glioblastoma activity of WHI-P154 in vitro is more than 200 fold amplified and selective by binding to recombinant human-derived epidermal growth factor. Malignant glioma cells were killed in vitro at a nanomolar concentration of EGF-P154 with an IC50 of 813 nM, but were not cytotoxic even at concentrations as high as 100 mM to leukemic cells that did not express EGF-R. WHI-P154 was the first inhibitor to inhibit only JAK3 but not JAK1 and JAK2. WHI-P154 inhibition of STAT1 activation, iNOS expression and NO production in macrophages in vitro. However, studies have shown that WHI-P154 can also inhibit other common kinases including EGFR, Src, Abl, VEGFR, MAPK and PI3-K and induce apoptosis in human glioblastoma cell lines. WHI-P154 inhibits adhesion and migration of malignant glioma cells in the presence of extracellular matrix (ECM). |
| In vivo study | In vivo use of EGF-P154 delayed tumor progression and improved disease-free survival in a glioblastoma xenograft model of severe combined immunodeficient mice. However, the survival time of tumor-free mice did not exceed 33 days (the median tumor-free survival was 19 days), and the tumor volume of tumor-free mice rapidly exceeded 500 in 58 days, 40% of mice treated with 1 mg/kg/day EGF-P154 for 10 consecutive days survived and no tumors were detected for more than 58 days, with a median tumor-free survival of 40 days. The tumor volume in the remaining 60% of mice never exceeded 50 mm3. In Vivo Use of EGF-P154 can delay tumor progression and improve disease-free survival in a glioblastoma xenograft model of severe combined immunodeficient mice. However, the survival time of tumor-free mice did not exceed 33 days (the median tumor-free survival was 19 days), and the tumor volume of tumor-free mice rapidly exceeded 500mm within 58 days. |
JAK3 Inhibitor - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
JAK3 Inhibitor - Introduction
WHI-P154 is an effective JAK3 inhibitor with an IC50 of 1.8 μM. It has no inhibitory activity on JAK1 and JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, and inhibits Stat3 instead of Stat5 phosphorylation.
Last Update：2022-10-16 17:41:34
JAK3 Inhibitor - Reference Information
| biological activity | WHI-P154 is an effective JAK3 inhibitor with IC50 of 1.8 μM, no inhibitory activity on JAK1 and JAK2, EGFR, Src, Abl, VEGFR and MAPK, Stat3 instead of Stat5 phosphorylation. WHI-P154 is an effective JAK3 inhibitor with an IC50 of 1.8 μM. It has no inhibitory activity on JAK1 and JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, and inhibits Stat3 instead of Stat5 phosphorylation. |
| in vitro study | WHI-P154 is the first inhibitor that only inhibits JAK3 but has no activity on JAK1 and JAK2. WHI-P154 inhibited STAT1 activation, iNOS expression, and NO production in macrophages in vitro. However, studies have proved that WHI-P154 can also inhibit other common kinases including EGFR, Src, Abl, VEGFR, MAPK and PI3-K and induce apoptosis in human malignant glioma cell lines. WHI-P154 inhibit adhesion and migration of malignant glioma cells in the presence of extracellular matrix (ECM). WHI-P154 has obvious cytotoxicity to human malignant glioma cell lines U373 and U87, and apoptosis can be induced at micromolar concentration. The anti-malignant glioma activity WHI-P154 in vitro is amplified by more than 200 times and is selective by binding to recombinant human epidermal growth factor. Malignant glioma cells were killed EGF-P154 at nanomolar concentrations in vitro with an IC50 of 813 nM, but there was no cytotoxicity to leukemic cells that did not express EGF-R even at concentrations as high as 100 mM. WHI-P154 is the first inhibitor that only inhibits JAK3 but has no activity on JAK1 and JAK2. WHI-P154 inhibited STAT1 activation, iNOS expression, and NO production in macrophages in vitro. However, studies have proved that WHI-P154 can also inhibit other common kinases including EGFR, Src, Abl, VEGFR, MAPK and PI3-K and induce apoptosis in human malignant glioma cell lines. WHI-P154 inhibit adhesion and migration of malignant glioma cells in the presence of extracellular matrix (ECM). |
| in vivo studies | in vivo use of EGF-P154 can delay tumor progression and improve the tumor-free survival rate of glioblastoma transplanted tumor model in severely combined immunodeficiency mice. However, the survival time of tumor-free mice did not exceed 33 days (the median tumor-free survival time was 19 days). The tumor volume of tumor-free mice would rapidly exceed 500 mm3 within 58 days. 40% of the mice treated with 1 mg/kg/day EGF-P154 for 10 days survived and no tumor was detected for more than 58 days. The median tumor-free survival time was 40 days. The tumor volume in the remaining 60% mice never exceeded 50 mm3. in vivo use of EGF-P154 can delay tumor progression and improve tumor-free survival rate of glioblastoma transplanted tumor model of severe combined immunodeficiency mice. However, the survival time of tumor-free mice did not exceed 33 days (the median tumor-free survival time was 19 days), and the tumor volume of tumor-free mice would rapidly exceed 500mm |
| target | TargetValue EGFR 4 nM VEGFR 100 nM Src 100 nM JAK3 () 1.8 μM |
| Target | Value |
| EGFR | 4 nM |
| VEGFR | 100 nM |
| Src | 100 nM |
| JAK3 () | 1.8 μM |
Last Update：2024-04-09 21:11:58
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Spot supply
Product Name: WHI-P154 Visit Supplier Webpage Request for quotationCAS: 211555-04-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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