R406 (free base)Syk inhibitor CAS# 841290-80-0 |
- R788 disodium
Catalog No.:BCC3695
CAS No.:1025687-58-4
- PRT062607 Hydrochloride
Catalog No.:BCC1869
CAS No.:1370261-97-4
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 841290-80-0 | SDF | Download SDF |
PubChem ID | 11213558 | Appearance | Powder |
Formula | C22H23FN6O5 | M.Wt | 470.4 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : ≥ 10 mg/mL (21.26 mM) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | ||
SMILES | CC1(C(=O)NC2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)C | ||
Standard InChIKey | NHHQJBCNYHBUSI-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C22H23FN6O5/c1-22(2)20(30)28-19-13(34-22)6-7-16(27-19)26-18-12(23)10-24-21(29-18)25-11-8-14(31-3)17(33-5)15(9-11)32-4/h6-10H,1-5H3,(H3,24,25,26,27,28,29,30) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | R406 (free base) is a potent inhibitor of Syk with IC50 of 41 nM. | |||||
Targets | Syk | |||||
IC50 | 41 nM |
R406 (free base) Dilution Calculator
R406 (free base) Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.1259 mL | 10.6293 mL | 21.2585 mL | 42.517 mL | 53.1463 mL |
5 mM | 0.4252 mL | 2.1259 mL | 4.2517 mL | 8.5034 mL | 10.6293 mL |
10 mM | 0.2126 mL | 1.0629 mL | 2.1259 mL | 4.2517 mL | 5.3146 mL |
50 mM | 0.0425 mL | 0.2126 mL | 0.4252 mL | 0.8503 mL | 1.0629 mL |
100 mM | 0.0213 mL | 0.1063 mL | 0.2126 mL | 0.4252 mL | 0.5315 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
R406 is a potent SYK inhibitorSpleen tyrosine kinase (SYK) is a non-receptor tyrosine kinase mainly expressed in hematopoietic cells. It transmits signals from a variety of cell surface receptors including CD74, Fc receptor and integrins. It is crucial for adaptive immune response, and also very important for cellular adhesion, innate immune recognition, osteoclast maturation, platelet activation and vascular development. [1]
Functional abnormality of SYK has been implicated in several blood malignancies. Constitutively active SYK can transform B cells. SYK inhibition can be beneficial for patients with blood cancers and autoimmune diseases.
R406 is a potent inhibitor of IgE and IgG mediated Fc receptor activation with EC50 for degranulation of 56-64 nM. [2] R406 targets SYK and inhibits phosphorylation of SYK substrates by binding to its ATP binding pocket and competing with ATP. R406 strongly inhibits SYK kinase activity with an IC50 of 41 nM.
R406 induces apoptosis in diffuse large B-cell lymphoma cell lines. It blocks B cell receptor signaling through inhibiton of SYK autophosphorylation of Y525/Y526 and SYK-dependent phosphorylation of the B-cell linker protein. [3]
R406 can be administrated orally.
References:
[1]Mocsai A, Ruland J, Tybulewicz VL. The SYK tyrosine kinase: a crucial player in diverse biological functions. Nat Rev Immunol 2010. 10(6): 387-402.
[2]Braselmann S, Taylor V, Zhao H, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther 2006. 319(3): 998-1008.
[3]Chen L, Monti S, Juszczynski P, et al. SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood 2008. 111(4): 2230*2237.
- Triptotriterpenic acid A
Catalog No.:BCN6780
CAS No.:84108-17-8
- Wilforlide A acetate
Catalog No.:BCN4384
CAS No.:84104-80-3
- Wilforlide A
Catalog No.:BCN4383
CAS No.:84104-71-2
- 1-Benzhydrylpiperazine
Catalog No.:BCC8453
CAS No.:841-77-0
- Roquinimex
Catalog No.:BCC5355
CAS No.:84088-42-6
- Lamotrigine
Catalog No.:BCC5051
CAS No.:84057-84-1
- Helioxanthin 8-1
Catalog No.:BCC5415
CAS No.:840529-13-7
- Fmoc-N-Me-Val-OH
Catalog No.:BCC3358
CAS No.:84000-11-3
- Fmoc-N-Me-Ala-OH
Catalog No.:BCC3210
CAS No.:84000-07-7
- Xanthoxyletin
Catalog No.:BCN6579
CAS No.:84-99-1
- Vitamin K1
Catalog No.:BCN2209
CAS No.:84-80-0
- Lapachol
Catalog No.:BCN4391
CAS No.:84-79-7
- R406
Catalog No.:BCC3876
CAS No.:841290-81-1
- 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride
Catalog No.:BCC8772
CAS No.:84163-13-3
- Ac-Glu(OtBu)-OH
Catalog No.:BCC2921
CAS No.:84192-88-1
- 7 8-Dihydroxy-4-Phenylcoumarin
Catalog No.:BCC8289
CAS No.:842-01-3
- Sudan I
Catalog No.:BCN8378
CAS No.:842-07-9
- Cyclosomatostatin
Catalog No.:BCC7693
CAS No.:84211-54-1
- Canagliflozin
Catalog No.:BCC3696
CAS No.:842133-18-0
- AKT Kinase Inhibitor
Catalog No.:BCC1335
CAS No.:842148-40-7
- Raclopride
Catalog No.:BCC7184
CAS No.:84225-95-6
- 5-O-Methylvisammioside
Catalog No.:BCN4954
CAS No.:84272-85-5
- Aliarin
Catalog No.:BCN3919
CAS No.:84294-77-9
- Pterosin D 3-O-glucoside
Catalog No.:BCN4567
CAS No.:84299-80-9