MedKoo Cat#: 206866 | Name: Gusacitinib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Gusacitinib, also known as ASN-002 and EN-3351, is a potent dual inhibitor of SYK/JAK kinases. ASN002 showed strong antitumor activity in both hematological and solid tumor xenograft models. ASN002 strongly suppressed the SYK and JAK family kinase signaling pathways as measured in pLAT and pSTAT assays, respectively. When profiled in a panel of 178 cell lines, ASN002 showed strong anti-proliferative activity in many lymphoid/leukemia cell lines, including SU-DHL-6, SU-DHL-4, OCI-LY10, H929 and Pfeiffer.

Chemical Structure

Gusacitinib
Gusacitinib
CAS#1425381-60-7 (free base)

Theoretical Analysis

MedKoo Cat#: 206866

Name: Gusacitinib

CAS#: 1425381-60-7 (free base)

Chemical Formula: C24H28N8O2

Exact Mass: 460.2335

Molecular Weight: 460.54

Elemental Analysis: C, 62.59; H, 6.13; N, 24.33; O, 6.95

Price and Availability

Size Price Availability Quantity
5mg USD 90.00 Ready to ship
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,350.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 3,750.00 2 Weeks
2g USD 6,250.00 2 Weeks
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Synonym
ASN002; ASN-002;ASN 002; EN3351, EN-3351; EN 3351; Gusacitinib;
IUPAC/Chemical Name
1-[5,6-Dihydro-4-[[4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5-oxopyrimido[4,5-d]pyridazin-2-yl]-4-piperidineacetonitrile
InChi Key
NLFLXLJXEIUQDL-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H28N8O2/c25-10-5-16-6-11-32(12-7-16)24-28-20-15-26-30-23(34)21(20)22(29-24)27-17-1-3-18(4-2-17)31-13-8-19(33)9-14-31/h1-4,15-16,19,33H,5-9,11-14H2,(H,30,34)(H,27,28,29)
SMILES Code
N#CCC1CCN(C2=NC(NC3=CC=C(N4CCC(O)CC4)C=C3)=C5C(C=NNC5=O)=N2)CC1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
IC50 of 5-46 nM in biochemical assays
Biological target:
Gusacitinib (ASN-002) is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 100.0 217.14
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 460.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1. http://cancerres.aacrjournals.org/content/77/13_Supplement/4204 2. Kinase Inhibitors for the Treatment of Immunological Disorders: Marian C. Bryan, and Naomi S. Rajapaksa; Publication Date (Web): June 5, 2018 (Perspective); DOI: 10.1021/acs.jmedchem.8b00667