Gusacitinib | ASN-002 | CAS#1425381-60-7 | SYK/JAK Kinase Inhibitor

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

MedKoo CAT#: 206866

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

Description: 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

CAS# 1425381-60-7 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206866
Name: Gusacitinib
CAS#: 1425381-60-7 (free base)
Chemical Formula: C24H28N8O2
Exact Mass: 460.23
Molecular Weight: 460.542
Elemental Analysis: C, 62.59; H, 6.13; N, 24.33; O, 6.95

Price and Availability

Size	Price	Availability
5mg	USD 90	Ready to ship
10mg	USD 150	Ready to ship
25mg	USD 250	Ready to ship
50mg	USD 450	Ready to ship
100mg	USD 750	Ready to ship
200mg	USD 1350	Ready to ship
500mg	USD 2650	Ready to ship
1g	USD 3750	2 Weeks
2g	USD 6250	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 2228989-14-6 (HCl) 1425381-60-7 (free base)

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

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#C21R02B09

QC Data:

View QC data: current batch, Lot#C21R02B09

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

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

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	100.0	217.14

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.

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

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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

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