| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
RO9021 (RO-9021) is a potent, orally bioavailavle, ATP-competative and selective inhibitor of spleen tyrosine kinase (SYK) with usefulness in autoimmune disease therapy, such as arthritis. It suppresses B-cell receptor signaling and inhibits SYK kinase activity with an average IC50 of 5.6 nM. An earlier investigation discovered that RO9021 could inhibit mouse bone marrow macrophage in vitro osteoclastogenesis in addition to suppressing Bcell receptor signaling in human peripheral blood mononuclear cells and whole blood, FcγR signaling in human monocytes, and Fc R signaling in human mast cells. Furthermore, it has been observed that RO9021 may inhibit the Toll-like Receptor 9 signaling in human B cells. This could result in a reduction of plasmablasts, immunoglobulin (Ig) G, and IgM levels following B-cell differentiation.
| Targets |
SYK (IC50 = 5.6 nM)
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Enzyme Assay |
Among the 392 kinases that have been tested, SYK is the only kinase that exhibits 99% competition with RO9021. RO9021 is a highly selective SYK inhibitor, with low S-scores of 0.003 for S(99) and 0.015 for S(90). As a result of blocking SYK kinase activity, RO9021 attenuates the downstream signaling cascade of the BCR. This is demonstrated by the fact that RO9021 inhibits the phosphorylation of BTK, PLCγ2, AKT, and ERK induced by antibodies.
|
|
| Cell Assay |
The human B-cell line Ramos was pretreated with 1 μM RO9021 before the BCR was cross-linked by an anti-IgM antibody. Using phosphospecific antibodies, a western blot was used to evaluate the activation of different BCR signaling components.
|
|
| Animal Protocol |
C57BL/6 and DBA/1J adult mice
5 and 45 mg/kg daily oral administration |
|
| References |
|
| Molecular Formula |
C18H25N7O
|
|
|---|---|---|
| Molecular Weight |
355.44
|
|
| Exact Mass |
355.212
|
|
| Elemental Analysis |
C, 60.82; H, 7.09; N, 27.58; O, 4.50
|
|
| CAS # |
1446790-62-0
|
|
| Related CAS # |
|
|
| PubChem CID |
71626896
|
|
| Appearance |
White to off-white solid powder
|
|
| Density |
1.3±0.1 g/cm3
|
|
| Boiling Point |
618.5±55.0 °C at 760 mmHg
|
|
| Flash Point |
327.9±31.5 °C
|
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
|
| Index of Refraction |
1.667
|
|
| LogP |
4.97
|
|
| Hydrogen Bond Donor Count |
4
|
|
| Hydrogen Bond Acceptor Count |
7
|
|
| Rotatable Bond Count |
5
|
|
| Heavy Atom Count |
26
|
|
| Complexity |
477
|
|
| Defined Atom Stereocenter Count |
2
|
|
| SMILES |
O=C(C1C(=C([H])C(=NN=1)N([H])[C@]1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[C@]1([H])N([H])[H])N([H])C1C([H])=C([H])C(C([H])([H])[H])=C(C([H])([H])[H])N=1)N([H])[H]
|
|
| InChi Key |
XJZVCDVZCRLIKN-QWHCGFSZSA-N
|
|
| InChi Code |
InChI=1S/C18H25N7O/c1-10-7-8-15(21-11(10)2)23-14-9-16(24-25-17(14)18(20)26)22-13-6-4-3-5-12(13)19/h7-9,12-13H,3-6,19H2,1-2H3,(H2,20,26)(H2,21,22,23,24)/t12-,13+/m0/s1
|
|
| Chemical Name |
6-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[(5,6-dimethylpyridin-2-yl)amino]pyridazine-3-carboxamide
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8134 mL | 14.0671 mL | 28.1341 mL | |
| 5 mM | 0.5627 mL | 2.8134 mL | 5.6268 mL | |
| 10 mM | 0.2813 mL | 1.4067 mL | 2.8134 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
