JANEX-1
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1350 | Check With Us |
| 500mg | $2160 | Check With Us |
| 1g | $3240 | Check With Us |
: Cat #: V3971 CAS #: 202475-60-3 Purity ≥ 98%
Description: JANEX-1 (aslo known as WHI-P131) is a novel, potent and selective inhibitor of the Janus kinase 3 (JAK3) that selectively inhibits JAK3 with an IC50 of 78 µM and does not inhibit JAK1 and JAK2.
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| Molecular Weight (MW) | 297.31 |
|---|---|
| Molecular Formula | C16H15N3O3 |
| CAS No. | 202475-60-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: ≥ 5 mg/mLr |
| Water: <1 mg/mLr | |
| Ethanol:<1 mg/mL | |
| SMILES Code | OC1=CC=C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1 |
| Synonyms | WHI-P131; WHI P-131; WHI P131; JANEX-1; JANEX 1; JANEX1 |
| Protocol | In Vitro | JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 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 EC50s 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 | 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 (ED50) 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%). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.3635 mL | 16.8175 mL | 33.6349 mL | 67.2699 mL |
| 5mM | 0.6727 mL | 3.3635 mL | 6.7270 mL | 13.4540 mL |
| 10mM | 0.3363 mL | 1.6817 mL | 3.3635 mL | 6.7270 mL |
| 20mM | 0.1682 mL | 0.8409 mL | 1.6817 mL | 3.3635 mL |
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Step One: Enter information below
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Average weight of animals g
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.