JAK3-IN-1
- Product Name
- JAK3-IN-1
- CAS No.
- 1805787-93-2
- Chemical Name
- JAK3-IN-1
- Synonyms
- JAK3-IN-1;JAK3 inhibitor 1;JAK-3-IN-1,JAK3 IN 1,JAK3IN1;2-Propenamide, N-[3-[[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]methyl]phenyl]-
- CBNumber
- CB63053896
- Molecular Formula
- C26H30ClN7O2
- Formula Weight
- 508.02
- MOL File
- 1805787-93-2.mol
JAK3-IN-1 Property
- Density
- 1.315±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 47 mg/mL (92.52 mM)
- form
- Solid
- pka
- 13.48±0.70(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-5283
- Product name
- JAK3-IN-1
- Purity
- 99.98%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
- Product number
- CS-5283
- Product name
- JAK3-IN-1
- Purity
- 99.98%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- orb611792
- Product name
- JAK3-IN-1
- Packaging
- 10mg
- Price
- $615.4
- Updated
- 2021/12/16
- Product number
- CS-5283
- Product name
- JAK3-IN-1
- Purity
- 99.98%
- Packaging
- 50mg
- Price
- $1800
- Updated
- 2021/12/16
- Product number
- orb611792
- Product name
- JAK3-IN-1
- Packaging
- 50mg
- Price
- $1802
- Updated
- 2021/12/16
JAK3-IN-1 Chemical Properties,Usage,Production
Uses
JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM)[1].
in vivo
JAK3-IN-1(Compound 9) shows reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng*hr/mL following a 10 mg/Kg oral dose and good oral bioavailability of 66%. After oral administration with JAK3-IN-1(Compound 9) (75 mpk, QD) for 8 days, the numbers of B or T lymphocytes in the tumor-bearing lungs and spleens of treated mice is not affected, however, the number of NK cells is reduced[1].
IC 50
JAK3: 4.8 nM (IC50); JAK1: 896 nM (IC50); JAK2: 1050 nM (IC50); TTK: 49 nM (IC50); BTK: 794 nM (IC50); ITK: 1070 nM (IC50)
References
[1] Tan L, et al. Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 2015 Aug 27;58(16):6589-6606. DOI:10.1021/acs.jmedchem.5b00710
JAK3-IN-1 Preparation Products And Raw materials
Raw materials
Preparation Products
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