ASN-002

Research use only, not for human use.

ASN-002 (Gusacitinib, ASN002) is a novel and potent dual inhibitor of SYK/JAK kinases with IC50 of 5-46 nM in biochemical assays.

ASN-002 (Gusacitinib, ASN002) is a novel and potent dual inhibitor of SYK/JAK kinases with IC50 of 5-46 nM in biochemical assays; strongly suppresses the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively; showed anti-proliferative activity in a broad panel of human cancer cell lines; exhibits significant efficacy in inhibiting tumor growth in a multiple myeloma (H929) xenograft model.Blood Cancer Phase 2 Clinical(In Vitro):In mechanistic cell-based studies involving IgE and cytokine stimulations, Gusacitinib (ASN-002) strongly suppresses the SYK and JAK family kinase signaling pathways measured as pLAT and pSTAT levels, respectively. Gusacitinib (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.(In Vivo):In a multiple myeloma (H929) xenograft model, Gusacitinib (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. Gusacitinib (ASN-002) has good oral bioavailability, metabolic stability, is not a Pgp substrate, and shows little to no inhibition of CYP450 isozymes. Gusacitinib (ASN-002) shows a favorable safety profile in rat and dog toxicology studies.

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Gusacitinib | ASN002

Angiogenesis

Syk

Syk

Cancer

Blood cancer

1425381-60-7

460.542

C24H28N8O2

>98% (HPLC)

DMSO : 100 mg/mL 217.14 mM

N#CCC1CCN(C2=NC(NC3=CC=C(N4CCC(O)CC4)C=C3)=C5C(C=NNC5=O)=N2)CC1

1-[5,6-Dihydro-4-[[4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5-oxopyrimido[4,5-d]pyridazin-2-yl]-4-piperidineacetonitrile

(-20℃)

With Ice Pack

≥ 2 years