Structure
JAK3-IN-1, inhibitor
JAK3-IN-1
Purity
98.00%
Synonyms
JAK3-IN-1; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 47mg/mL (92.52mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C26H30ClN7O2
SMILES
O=C(C=C)NC1=CC(CNC2=NC(NC3=C(OC)C=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=CC=C1
CAS Number
1805787-93-2
Target & IC50
JAK3: ic50 4.8nM
JAK1: ic50 896nM
JAK2: ic50 1050nM
TTK: ic50 49nM
BTK: ic50 794nM
ITK: ic50 1070nM
JAK1: ic50 896nM
JAK2: ic50 1050nM
TTK: ic50 49nM
BTK: ic50 794nM
ITK: ic50 1070nM
In Vitro
The numbers of B or T lymphocytes in the tumor-bearing lungs and spleens of treated mice is not affected, after oral administration with JAK3-IN-1(Compound 9) (75mpk, QD) for 8 days, however, the number of NK cells is reduced. JAK3-IN-1 displays reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng*hr/mL following a 10mg/Kg oral dose and good oral bioavailability of 66% [1].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for JAK3-IN-1, inhibitor
JAK3-IN-1 is a selective and orally active JAK3 inhibitor (IC50: 4.8nM). JAK3-IN-1 displays over 180-fold more selective for JAK3 than JAK1 (IC50: 896nM) and JAK2 (IC50: 1050nM).
Product Categories/Family for JAK3-IN-1, inhibitor
References
Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606.
Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606.
Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606.
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Product Notes
The JAK3-IN-1 (Catalog #AAA5755014) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "JAK3-IN-1, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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