202475-60-3
JANEX-1
CAS: 202475-60-3
Molecular Formula: C16H15N3O3
202475-60-3 - Names and Identifiers
| Name | JANEX-1 |
| Synonyms | Janex 1 JANEX-1 WHI-P131 JAK3 INHIBITOR I WHI-P131(Janex 1) A JAK3 inhibitorWHI-P131 4-(6,7-dimethoxyquinazolin-4-ylamino)phenol 4-(4'-HYDROXYPHENYL)AMINO-6,7-DIMETHOXYQUINAZOLINE |
| CAS | 202475-60-3 |
202475-60-3 - Physico-chemical Properties
| Molecular Formula | C16H15N3O3 |
| Molar Mass | 297.31 |
| Density | 1.336±0.06 g/cm3(Predicted) |
| Boling Point | 468.1±40.0 °C(Predicted) |
| Solubility | DMSO: 18mg/mL, soluble |
| Appearance | solid |
| Color | yellow |
| pKa | 10.06±0.26(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Protect from moisture. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| In vitro study | JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC 50 of 78 μM), does not inhibit JAK1 and JAK2, the ZAP/SYK family tyrosine kinase SYK, the TEC family tyrosine kinase BTK, the SRC family tyrosine kinase LYN, or the receptor family tyrosine kinase insulin receptor kinase, even at concentrations as high as 350 μM. JANEX-1 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19 but not in melanoma (M24-MET) or squamous carcinoma (SQ20B) cells. WHI-P131 inhibits the clonogenic growth of JAK3-positive leukemia cell lines DAUDI, RAMOS, LC1;19, NALM-6, MOLT-3, and HL-60 (but not JAK3-negative BT-20 breast cancer, M24-MET melanoma, or SQ20B squamous carcinoma cell lines) in a concentration-dependent fashion. WHI-P131 inhibits clonogenic growth in a concentration-dependent fashion with EC 50 s of 24.4 μM for NALM-6 cells and 18.8 μM for DAUDI cells. At 100 μM, WHI-P131 inhibits the in vitro colony formation by these leukemia cell lines by >99%. In contrast, JANEX-1 does not inhibit the clonogenic growth of JAK3-negative M24-MET melanoma or SQ20B squamous carcinoma cell lines. |
| In vivo study | JANEX-1 is administered at doses ranging from 5 to 100 mg/kg. Evaluation of CPK activity revealed a dose-response curve with an effective dose 50 (ED 50 ) value of 7.44 mg/kg. Mice receiving JANEX-1 displayed significantly reduced CPK and LDH levels. In addition, the infarct size of JANEX-1-treated mice (30.16±2.79%) is significantly decreased when compared with I/R-operated mice (65.64±3.76%). JANEX-1 (WHI-P131) is absorbed rapidly, and the time to reach the maximum plasma JANEX-1 concentration (t max ) is 24.7±1.7 min. JANEX-1 is rapidly eliminated with an elimination half-life of 45.6±5.5 min. Although the predicted maximum plasma JANEX-1 concentration is 10.5 ± 0.8 μM, which is only half of the C max following i.v. administration of the same bolus dose, the i.p. bioavailability is 94.6% and the systemic exposure levels (i.e., AUC) are very similar to those observed after i.v. injection (17.1±2.2 μM•h versus 18.1±1.2 μM•h). |
202475-60-3 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
202475-60-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.363 ml | 16.817 ml | 33.635 ml |
| 5 mM | 0.673 ml | 3.363 ml | 6.727 ml |
| 10 mM | 0.336 ml | 1.682 ml | 3.363 ml |
| 5 mM | 0.067 ml | 0.336 ml | 0.673 ml |
Last Update：2024-01-02 23:10:35
202475-60-3 - Reference Information
| biological activity | JANEX-1 (WHI-P131) is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 with an IC50 of 78 μm. It did not affect the activity of JAK1 or JAK2, and other protein tyrosine kinases (IC50> 350 µm). |
| Target | Value |
| JAK3 (Cell-free assay) | 78 μM |
Last Update：2024-04-09 20:49:11
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Spot supply
Product Name: JANEX-1 Visit Supplier Webpage Request for quotationCAS: 202475-60-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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