ASN-002|Gusacitinib|CAS 1425381-60-7|DC Chemicals

Cas No.:	1425381-60-7
Chemical Name:	Gusacitinib
Synonyms:	Gusacitinib;ASN002;ASN-002;ASN 002
SMILES:	N#CCC1CCN(C2=NC(NC3=CC=C(N4CCC(O)CC4)C=C3)=C5C(C=NNC5=O)=N2)CC1
Formula:	C₂₄H₂₈N₈O₂
M.Wt:	460.542
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Sanjeeva Reddy, et al. Abstract 792: ASN002: A novel dual SYK/JAK inhibitor with strong antitumor activity. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.

Description:	ASN-002 is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM.
Target:	IC50: 5-46 nM (SYK, JAK)[1].
In Vivo:	In a multiple myeloma (H929) xenograft model, ASN-002 exhibits significant efficacy in inhibiting tumor growth (>95%). It also significantly delays the onset of hind limb paralysis in the human erythroleukemia (HEL) mouse model. ASN-002 has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. ASN-002 shows a favorable safety profile in rat and dog toxicology studies[1].
In Vitro:	In mechanistic cell-based studies involving IgE and cytokine stimulations, ASN-002 strongly suppresses the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively. ASN-002 shows anti-proliferative activity in a broad panel of human cancer cell lines including DHL6, DHL4, OCI-LY10, H929, Pfeiffer, HT-1376, and Lovo, suggesting activity in both solid and hematological tumor types[1].
References:	[1]. Sanjeeva Reddy, et al. Abstract 792: ASN002: A novel dual SYK/JAK inhibitor with strong antitumor activity. AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA.

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Gusacitinib (ASN-002)