MedKoo Cat#: 576007 | Name: Lanraplenib succinate

Description:

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

Lanraplenib, also known as GS-9876 and GS-SYK, is a tyrosine kinase inhibitor. Lanraplenib blocked the progression of LN-like disease in NZB/W mice. Human in vitro and murine in vivo data suggest that lanraplenib may be efficacious in preventing disease progression in patients with LN at least in part by inhibiting B cell maturation. GS-9876 inhibited SYK activity in platelets via the GPVI receptor without prolonging BT in monkeys or humans. Furthermore, GS-9876 did not increase inhibition of platelet aggregation by NSAIDs in vitro, suggesting that these agents can potentially be combined without increasing bleeding risk in humans.

Chemical Structure

Lanraplenib succinate
Lanraplenib succinate
CAS#1800047-00-0 (succinate)

Theoretical Analysis

MedKoo Cat#: 576007

Name: Lanraplenib succinate

CAS#: 1800047-00-0 (succinate)

Chemical Formula: C58H68N18O14

Exact Mass: 1240.5162

Molecular Weight: 1241.29

Elemental Analysis: C, 56.12; H, 5.52; N, 20.31; O, 18.04

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
GS-SYK, GS-9876; GS 9876; GS9876; Lanraplenib succinate
IUPAC/Chemical Name
Butanedioic acid, compd. with 6-(6-amino-2-pyrazinyl)-N-(4-(4-(3-oxetanyl)-1-piperazinyl)phenyl)imidazo(1,2-a)pyrazin-8-amine (3:2)
InChi Key
SUXNLHAGYIRFJQ-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
Nc1cncc(n1)c2cn3ccnc3c(Nc4ccc(cc4)N5CCN(CC5)C6COC6)n2.Nc7cncc(n7)c8cn9ccnc9c(Nc%10ccc(cc%10)N%11CCN(CC%11)C%12COC%12)n8.OC(=O)CCC(=O)O.OC(=O)CCC(=O)O.OC(=O)CCC(=O)O
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
Solvent mg/mL mM
Solubility
Soluble in DMSO 0.0 100.00
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 1,241.29 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
1: Németh T, Balogh L, Káposztás E, Szilveszter KP, Mócsai A. Neutrophil- specific Syk expression is crucial for skin disease in experimental epidermolysis bullosa acquisita. J Invest Dermatol. 2023 Jan 11:S0022-202X(23)00010-6. doi: 10.1016/j.jid.2022.12.016. Epub ahead of print. PMID: 36641133. 2: Price E, Bombardieri M, Kivitz A, Matzkies F, Gurtovaya O, Pechonkina A, Jiang W, Downie B, Mathur A, Mozaffarian A, Mozaffarian N, Gottenberg JE. Safety and efficacy of filgotinib, lanraplenib and tirabrutinib in Sjögren's syndrome: a randomized, phase 2, double-blind, placebo-controlled study. Rheumatology (Oxford). 2022 Nov 28;61(12):4797-4808. doi: 10.1093/rheumatology/keac167. PMID: 35377447; PMCID: PMC9707320. 3: Tang S, Yu Q, Ding C. Investigational spleen tyrosine kinase (SYK) inhibitors for the treatment of autoimmune diseases. Expert Opin Investig Drugs. 2022 Mar;31(3):291-303. doi: 10.1080/13543784.2022.2040014. Epub 2022 Feb 18. PMID: 35130124. 4: Werth VP, Fleischmann R, Robern M, Touma Z, Tiamiyu I, Gurtovaya O, Pechonkina A, Mozaffarian A, Downie B, Matzkies F, Wallace D. Filgotinib or lanraplenib in moderate to severe cutaneous lupus erythematosus: a phase 2, randomized, double-blind, placebo-controlled study. Rheumatology (Oxford). 2022 May 30;61(6):2413-2423. doi: 10.1093/rheumatology/keab685. PMID: 34498056; PMCID: PMC9157055. 5: Pohlmeyer CW, Shang C, Han P, Cui ZH, Jones RM, Clarke AS, Murray BP, Lopez DA, Newstrom DW, Inzunza MD, Matzkies FG, Currie KS, Di Paolo JA. Characterization of the mechanism of action of lanraplenib, a novel spleen tyrosine kinase inhibitor, in models of lupus nephritis. BMC Rheumatol. 2021 Mar 30;5(1):15. doi: 10.1186/s41927-021-00178-3. PMID: 33781343; PMCID: PMC8008554. 6: Baker M, Chaichian Y, Genovese M, Derebail V, Rao P, Chatham W, Bubb M, Lim S, Hajian H, Gurtovaya O, Patel U, Tumlin J. Phase II, randomised, double-blind, multicentre study evaluating the safety and efficacy of filgotinib and lanraplenib in patients with lupus membranous nephropathy. RMD Open. 2020 Dec;6(3):e001490. doi: 10.1136/rmdopen-2020-001490. PMID: 33380521; PMCID: PMC7780527. 7: Blomgren P, Chandrasekhar J, Di Paolo JA, Fung W, Geng G, Ip C, Jones R, Kropf JE, Lansdon EB, Lee S, Lo JR, Mitchell SA, Murray B, Pohlmeyer C, Schmitt A, Suekawa-Pirrone K, Wise S, Xiong JM, Xu J, Yu H, Zhao Z, Currie KS. Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases. ACS Med Chem Lett. 2020 Feb 12;11(4):506-513. doi: 10.1021/acsmedchemlett.9b00621. PMID: 32292557; PMCID: PMC7153012.