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Entospletinib (GS-9973)

Name: Entospletinib (GS-9973)
Brand: Selleck Chemicals
SKU: S7523
Rating: 5 (33 reviews)

Catalog No.S7523

For research use only.

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.

Entospletinib (GS-9973) Chemical Structure

CAS No. 1229208-44-9

Selleck's Entospletinib (GS-9973) has been cited by 33 publications

Purity & Quality Control

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Syk Signaling Pathway Map

Biological Activity

Description

Features

Orally bioavailable Syk-selective inhibitor that has been tested in Phase II clinical trials for treatment of Haematological Malignancies.

Targets

Syk ^[1]
(Cell-free assay)

7.7 nM

In vitro

GS-9973 shows good bidirectional permeability across Caco-2 cell monolayers in vitro. In cells, GS-9973 also shows excellent selectivity for Syk, and potently inhibits BCR-mediated activation and proliferation of B-cells as well as immune-complex-stimulated cytokine production in monocytes. ^[1] The combination of idelalisib and GS-9973 synergistically inhibits CLL cell viability and further disrupts chemokine signaling. ^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

human MV411 cells	MmHyVJJwdGmoZYLheIlwdiCjc4PhfS=>	MYq3NkBp	M334[2lvcGmkaYTpc44hd2ZiRnz0N{BqdiCqdX3hckBOXjRzMTDj[YxteyCjc4Pld5Nm\CCjczDhd5Nme3OnZDDhd{Bxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BqdmO3YnH0bY9vKGK7IIPw[YN1em:yaH;0c41mfHK7LDDFR\|UxRTBwM{K3JO69VQ>?	Ml3zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{m1NVQoRjJ2N{e5OVE1RC:jPh?=
C57BL/6 mouse bone marrow cells	MUTDfZRwfG:6aXRCpIF{e2G7	NGPj[JE1KGSjeYO=	MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBEPTeETD:2JI1wfXOnIHLvcoUhdWG{cn;3JINmdGy\|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJJBz\WmwY4XiZZRm\CCob4KgOEBl[Xm\|IH\vcIxwf2WmIHL5JHs{UF1vdHj5cYllcW6nIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDViaILzJIJ6KGKndHHwcIF1\SClb4XueIlv\yCjbnHsfZNqeyxiSVO1NF0xNjV6MjFOwG0>	NX;NW5pZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2N\|M4PDFpPkK1OlM{PzRzPD;hQi=>
Ramos cells	MkPjSpVv[3Srb36gZZN{[Xl?		M4r5fWlvcGmkaYTpc44hd2ZiU4nrJIlvKGGwdHnoeY1idiCLZ12td5RqdXWuYYTl[EBpfW2jbjDSZY1weyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDCR3IudWWmaXH0[YQhSkyQSzDwbI9{eGixconsZZRqd25iYomgZ4VtdHWuYYKgZZN{[XluIFXDOVA:OC5yMkdOwG0>	NFvBe489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVUyPCd-MkS3O\|k2OTR:L3G+
B-cells	NV25boxqTnWwY4Tpc44h[XO\|YYm=	M3XIVVEhcHJ?	Ml3OTY5pcWKrdHnvckBw\iCVeXugbY4h[WyyaHHJ[20ue3SrbYXsZZRm\CCqdX3hckBDKGOnbHzzJIF{e2W\|c3XkJIF{KGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkAyKGi{IHnuZ5Vj[XSrb36gZpkh\myxdzDjfZRwdWW2comsJGVEPTB;MD6wOFHPxE1?	MlK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{m1NVQoRjJ2N{e5OVE1RC:jPh?=
B-cells	M{nzcGZ2dmO2aX;uJIF{e2G7	NInBT2oyKGi{	NIjGSIFKdmirYnn0bY9vKG:oIGP5b{BqdiCjbIDoZWloVS2\|dHnteYxifGWmIHj1cYFvKEJiY3XscJMh[XO\|ZYPz[YQh[XNiQ1S4OkBmgHC{ZYPzbY9vKGGodHXyJFEhcHJiaX7jeYJifGmxbjDifUBndG:5IHP5eI9u\XS{eTygSWM2OD1yLkGyOe69VQ>?	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd5OUWxOEc,OjR5N{m1NVQ9N2F-
mast cells	MYnGeY5kfGmxbjDhd5NigQ>?	Mn\1NUBpeg>?	NIHX[I5KdmirYnn0bY9vKG:oIHPLbZQhcW5ic4TlcUBk\WyuIH\hZ5Rwei2\|dHnteYxifGWmIHLvcoUhdWG{cn;3JIRmemm4ZXSgcY92e2VibXHzeEBk\WyuczDhd5Nme3OnZDDhd{BxcG:\|cHjvdplt[XSrb36gZYZ1\XJiMTDodkBqdmO3YnH0bY9vNCCHQ{WwQVAvPDR3zszN	NGqybVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe3PVUyPCd-MkS3O\|k2OTR:L3G+
TF1	M1LUOmZ2dmO2aX;uJIF{e2G7	NEKyeFcyKGi{	NE[weGxKdmirYnn0bY9vKG:oIFrhb\|IhcW5iZYL5eIhzd3CxaXX0bY4ue3SrbYXsZZRm\CCqdX3hckBVTjFiY3XscJMh[XO\|ZYPz[YQh[XNiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3TeIF1PSCjZoTldkAyKGi{IHnuZ5Vj[XSrb36sJGVEPTB;MD60OVPPxE1?	MmDKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5N{m1NVQoRjJ2N{e5OVE1RC:jPh?=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot

p-ERBB2 / ERBB2 / pEGFR / EGFR ; SYK / p-SYK

31492560 29537660

In vivo

GS-9973 (1 mg/kg p.o.) shows moderate to high bioavailability in rat and dog. In a rat collagen-induced arthritis model, GS-9973 (1-10 mg/kg p.o.) significantly inhibits ankle inflammation. Moreover, GS-9973 also shows disease-modifying activity in multiple histological measurements, including inhibition of pannus formation, cartilage damage, bone resorption, and peritosteal bone formation with ED50 ranging from 1.2 to 3.9 mg/kg . ^[1]

Protocol (from reference)

Kinase Assay: ^[1]	Kinase Assays: Full-length baculovirus-expressed Syk kinase activity is measured in a Lance-based assay format in a final volume of 25 μL containing 25 mM Tris–HCl, pH 7.5, 5 mM β-glycerophosphate, 2 mM DTT, 0.1 mM Na₃VO₄, 10 mM MgCl₂, 0.5 μM Promega PTK biotinylated peptide substrate 1, 0.01% casein, 0.01% Triton X-100, 0.25% glycerol, and 40 mM ATP (Km for ATP) incubated at room temperature for 60 min. Reactions are stopped with the addition of 30 mM EDTA containing 30 μL of SA-APC and 4 nM PT-66 antibody and the plates measured on a Perkin-Elmer Envision. IC50 values for test compounds are determined using a four-parameter linear regression algorithm.
Cell Research: ^[1]	Cell lines: MV-4-11 cells Concentrations: ~10 μM Incubation Time: 72 hours Method: Functional impact on cellular Flt3 activity is determined by measuring compound inhibition of MV-4-11 cell proliferation. A total of 104 cells are diluted in RPMI medium containing 10% FBS in 96-well flat-bottomed tissue culture plates and incubated with compound dilutions for 72 h at 37 癈. Alamar blue (10%) is added to the cells, which were incubated for an additional 12-18 h at 37 癈, and inhibition of the relative cell numbers is determined by spectrophotometer readings at 570/600 nm.
Animal Research: ^[1]	Animal Models: Rat Collagen-Induced Arthritis (CIA) Model Dosages: ~10 mg/kg bid Administration: p.o.

References

Solubility (25°C)

In vitro	DMSO	26 mg/mL warmed (63.18 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 4% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing. Click to purchase: PEG300 Tween 80	2.5mg/mL

Chemical Information

Molecular Weight	411.46
Formula	C₂₃H₂₁N₇O
CAS No.	1229208-44-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1COCCN1C2=CC=C(C=C2)NC3=NC(=CN4C3=NC=C4)C5=CC6=C(C=C5)C=NN6

Download Entospletinib (GS-9973) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
How should we use S7523 to perform intraperitoneal injection in mice?

Answer:
S7523 can be dissolved in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at up to 2.5mg/ml and use it for intra peritoneal injection in mice. When making this vehicle, please dissolve the product in DMSO first, then add PEG 300 and Tween 80 and dilute with water as a final step.

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