1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. Lanraplenib succinate

Lanraplenib succinate (Synonyms: GS-9876 succinate)

Cat. No.: HY-109091B
Handling Instructions

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.

For research use only. We do not sell to patients.

Lanraplenib succinate Chemical Structure

Lanraplenib succinate Chemical Structure

CAS No. : 1800047-00-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 437 In-stock
Estimated Time of Arrival: December 31
1 mg USD 105 In-stock
Estimated Time of Arrival: December 31
5 mg USD 320 In-stock
Estimated Time of Arrival: December 31
10 mg USD 520 In-stock
Estimated Time of Arrival: December 31
25 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target

IC50: 9.5 nM (SYK)[1]

In Vitro

Lanraplenib succinate (GS-9876 succinate) inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells with EC50 values of 24-51 nM. Lanraplenib monosuccinate inhibits anti-IgM mediated CD69 and CD86 expression on B-cells (EC50=112±10 nM and 164±15 nM, respectively) and anti-IgM /anti-CD40 co-stimulated B cell proliferation (EC50=108±55 nM). In human macrophages, Lanraplenib succinate inhibits IC-stimulated TNFα and IL-1β release (EC50=121±77 nM and 9±17 nM, respectively)[1].
Lanraplenib succinate (GS-9876 succinate) inhibits glycoprotein VI (GPVI)-induced phosphorylation of linker for activation of T cells and phospholipase Cγ2, platelet activation and aggregation in human whole blood, and platelet binding to collagen under arterial flow[2].

Molecular Weight

620.64

Formula

C₂₃H₂₅N₉O.₃/₂C₄H₆O₄

CAS No.

1800047-00-0

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.[3/2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (134.26 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6112 mL 8.0562 mL 16.1124 mL
5 mM 0.3222 mL 1.6112 mL 3.2225 mL
10 mM 0.1611 mL 0.8056 mL 1.6112 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.35 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.35 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LanraplenibGS-9876GS9876GS 9876SykSpleen tyrosine kinaseInhibitorinhibitorinhibit

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Product name:
Lanraplenib succinate
Cat. No.:
HY-109091B
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