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Lanraplenib (succinate)

CAT: 0804-HY-109091B-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-109091B-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans[1][2][3].
CAS Number
1800047-00-0
Product Name Alternative
GS-9876 (succinate)
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Syk
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Neuroscience-Neuromodulation
Field of Research
Inflammation/Immunology; Cancer
Assay Protocol
https://www.medchemexpress.com/lanraplenib-succinate.html
Purity
98.09
Solubility
DMSO : 83.33 mg/mL (ultrasonic)
Smiles
NC1=CN=CC(C2=CN3C(C(NC4=CC=C(N5CCN(C6COC6)CC5)C=C4)=N2)=NC=C3)=N1.O=C(O)CCC(O)=O
Molecular Formula
C23H25N9O.3/2C4H6O4
Molecular Weight
620.64
Precautions
H302, H315, H319, H335
References & Citations
[1]Di Paolo J, et al. FRI0049 Preclinical Characterization of GS-9876, A Novel, Oral SYK Inhibitor That Shows Efficacy in Multiple Established Rat Models of Collagen-Induced Arthritis.Annals of the Rheumatic Diseases 2016;75:443-444.|[2]Clarke AS, et al. Effects of GS-9876, a novel spleen tyrosine kinase inhibitor, on platelet function and systemic hemostasis. Thromb Res. 2018 Oct;170:109-118.|[3]Kivitz AJ, et al. GS-9876, a Novel, Highly Selective, SYK Inhibitor in Patients with Active Rheumatoid Arthritis: Safety, Tolerability and Efficacy Results of a Phase 2 Study [abstract]. Arthritis Rheumatol.2018; 70 (suppl 10) .
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 2

Chemical Information

Lanraplenib Succinate

Lanraplenib Succinate is the succinate salt form of lanraplenib, an orally available inhibitor of spleen tyrosine kinase (Syk), with potential immunomodulating and antineoplastic activities. Upon oral administration, lanraplenib binds to and inhibits the activity of Syk. This inhibits B-cell receptor (BCR) signaling, which leads to the inhibition of B-cell activation, and prevents tumor cell activation, migration, adhesion and proliferation. Syk, a non-receptor cytoplasmic, BCR-associated tyrosine kinase, is expressed in hematopoietic tissues and is often overexpressed in hematopoietic malignancies; it plays a key role in B-cell receptor signaling.

CAS Number1800047-00-0
PubChem CID133082362
IUPAC Namebis(6-(6-aminopyrazin-2-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine);tris(butanedioic acid)
Molecular FormulaC58H68N18O14
Molecular Weight1241.3
Topological Polar Surface Area443
Hydrogen Bond Donor Count10
Hydrogen Bond Acceptor Count30
Rotatable Bond Count19
Heavy Atom Count90
Formal Charge0
Complexity728
SMILES
C1CN(CCN1C2COC2)C3=CC=C(C=C3)NC4=NC(=CN5C4=NC=C5)C6=CN=CC(=N6)N.C1CN(CCN1C2COC2)C3=CC=C(C=C3)NC4=NC(=CN5C4=NC=C5)C6=CN=CC(=N6)N.C(CC(=O)O)C(=O)O.C(CC(=O)O)C(=O)O.C(CC(=O)O)C(=O)O
InChI
InChI=1S/2C23H25N9O.3C4H6O4/c2*24-21-12-25-11-19(28-21)20-13-32-6-5-26-23(32)22(29-20)27-16-1-3-17(4-2-16)30-7-9-31(10-8-30)18-14-33-15-18;3*5-3(6)1-2-4(7)8/h2*1-6,11-13,18H,7-10,14-15H2,(H2,24,28)(H,27,29);3*1-2H2,(H,5,6)(H,7,8)
InChIKey
SUXNLHAGYIRFJQ-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Lanraplenib Succinate
CAS: 1800047-00-0
CID: 133082362
Formula: C58H68N18O14
MW: 1241.3
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight1241.3
Hydrogen Bond Donor Count10
Hydrogen Bond Acceptor Count30
Rotatable Bond Count19
Exact Mass1240.51623892
Monoisotopic Mass1240.51623892
Topological Polar Surface Area443 Ų
Heavy Atom Count90
Formal Charge0
Complexity728
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count5
Compound Is CanonicalizedYes

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