[CAS NO. 1446790-62-0] RO9021
PRODUCTS SPECIFICATIONS [1446790-62-0]
DESCRIPTION [1446790-62-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 355.44 |
| Molecular Formula | C18H25N7O |
| SMILES | NC(C1=C(NC2=CC=C(C)C(C)=N2)C=C(N[C@H]3[C@@H](N)CCCC3)N=N1)=O |
Summary
RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK , with an average IC 50 of 5.6 nM.
IC50 & Target
IC50: 5.6 nM (SYK)
In Vitro
RO9021 is a highly selective SYK inhibitor with low S-scores of 0.003 for S(99) and 0.015 for S(90), indicating that SYK is the only kinase with 99% competition with RO9021 in a total of 392 tested kinases. RO9021 inhibits anti-IgM induced phosphorylation of BTK, PLCγ2, AKT and ERK, indicating that blockade of SYK kinase activity by RO9021 results in attenuation of BCR downstream signaling cascade. RO9021 selectively suppresses B-cell receptor signaling. RO9021 also displays a similar inhibitory potency (IC 50 =22.8±1.7 nM) in a FcεR-mediated mast cell activation and degranulation assay [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 3.03 mg/mL ( 8.52 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 | --- | --- | --- |