RO0921|RO-0921|SYK inhibitor

Cas No.:	1446790-62-0
Chemical Name:	RO-0921,RO 0921
Synonyms:	RO-0921,RO 0921
SMILES:	C(NC1=CC(N[C@@H]2[C@H](N)CCCC2)=NN=C1C(=O)N)1=CC=C(C)C(C)=N1
Formula:	C₁₈H₂₅N₇O
M.Wt:	355.44
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.

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 (IC50=22.8±1.7 nM) in a FcεR-mediated mast cell activation and degranulation assay[1].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC70457	GSK2646264	GSK2646264 (GSK-2646264) is a potent, selective Spleen Tyrosine Kinase (Syk) inhibitor with pIC50 of 7.1, >300-fold selectivity over Autota B; inhibits anti-IgM induced Erk1/2 phosphorylation in Ramos B cells with pIC50 of 6.7.
DC10523	TAK-659 HCl	TAK-659 hydrochloride is a potent, selective and orally available spleen tyrosine kinase (Syk) inhibitor with an IC50 of 3.2 nM.
DC9759	RO0921	RO0921 is a novel, potent SYK inhibitor.
DC1013	R788 disodium (Fostamatinib)	R935788 (Fostamatinib disodium, R788) is a Syk inhibitor with IC50 of 41 nM.
DC9841	Fostamatinib(R788)	R788 (Fostamatinib), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.
DC8733	R406	R406 is a potent Syk inhibitor with IC50 of 41 nM and also potently inhibits Flt3.
DC1014	R406 free base	R406 is a potent Syk inhibitor with IC50 of 41 nM and also potently inhibits Flt3.
DC10660	BAY 61-3606 free base	BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.
DC9632	BAY 61-3606 (dihydrochloride)	BAY 61-3606 2Hcl is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.