R406 free base

Name: R406 free base
Brand: MedChemExpress
SKU: HY-11108
Rating: 5.0 (36 reviews)

製品番号: HY-11108 純度: 99.07%: Data Sheet SDS COA 取扱説明書
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R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM).

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CAS 番号 : 841290-80-0

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 83	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 83	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$50	在庫あり	Estimated Time of Arrival: December 31
5 mg	$80	在庫あり	Estimated Time of Arrival: December 31
10 mg	$130	在庫あり	Estimated Time of Arrival: December 31
25 mg	$254	在庫あり	Estimated Time of Arrival: December 31
50 mg	$430	在庫あり	Estimated Time of Arrival: December 31
100 mg	$680	在庫あり	Estimated Time of Arrival: December 31
250 mg	$992	在庫あり	Estimated Time of Arrival: December 31
500 mg	$1200	在庫あり	Estimated Time of Arrival: December 31
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Based on 36 publication(s) in Google Scholar

Other Forms of R406 free base:

R406 在庫あり

顧客検証

Cell Migration/Invasion Assay

Flow Cytometry

: R406 free base purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Apr 19;13(1):2136. [Abstract]; Comparison of pharmacological inhibitors with the corresponding guides of positive and negative controls for BCR-controlled adhesion. Top plots: Namalwa cells pretreated with 100 nM ibrutinib (BTK inhibitor), 1 μM R406 (Fostamatinib, SYK inhibitor, 1 ), 100 nM wortmannin (pan-PI3K inhibitor), 50 μM PD-98059 (MEK1/2 inhibitor), 2.5 μM MK-2206 (AKT1/2/3 inhibitor), or DMSO control, were stimulated with αIgM or PMA, and allowed to adhere to fibronectin-coated surfaces. Bar graphs are presented as normalized mean + SEM (100% = untreated αIgM-stimulated cells). Bottom plots: MA plots of αIgM-induced adhesion relative to PMA-induced adhesion; the guides of the corresponding genes targeted by the inhibitors of the top plots are highlighted.

: R406 free base purchased from MedChemExpress. Usage Cited in: Exp Hematol Oncol. 2022 Nov 8;11(1):88. [Abstract]; R406 (1-2 μM; 18-24 h) markedly inhibited C. tropicalis-induced PKM2 Tyr105 phosphorylation and PKM2 nuclear translocation in MDSCs by suppressing Syk.

: R406 free base purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 May 24;11(15):7308-7321. [Abstract]; The induction of IL-21 secretion by CBP-12-OVA was inhibited by R406, an inhibitor of Syk phosphorylation. FL-DCs were incubated with 2.5 µM R406 for 1 h, and then cultured with 100 µg/mL of the indicated peptides for 6 h at 37 °C. IL-21 positive frequency was determined by ICS assay.

: R406 free base purchased from MedChemExpress. Usage Cited in: Cell. 2018 Oct 4;175(2):442-457.e23. [Abstract]; Syk inhibitors (R406 (5 μM) and Piceatannol) are added during the induction of trastuzumab-dependent BT-474 phagocytosis. The binding of the phagosome marker Rab7 to AIM2 in macrophages are evaluated by co-immunoprecipitation.

: R406 free base purchased from MedChemExpress. Usage Cited in: J Pharmacol Sci. 2017 May;134(1):29-36. [Abstract]; The effects of R406 treatment on the phosphorylation of 3BP2 and p38MAPK in white blood cells from the spleens of NZB/W F1 mice. (A) The phosphorylation of the 3BP2 and (B) the phosphorylation of p38MAPK in the renal cortex of control and R406-treated mice.

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製品説明

R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 free base reduces immune complex-mediated inflammation^[1]. R406 free base also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM)^[2].

IC₅₀ & Target

Ki: 30 nM (Syk)^[1]
IC50: 41 nM (Syk)^[1]
FLT3^[1]
IC50: 63 nM (Lyn), 37 nM (Lck)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	IC₅₀	147 1 Compound: 2	Inhibition of IL3 dependent proliferation in C57/B16 mouse bone marrow cells using [3H]thymidine by liquid scintillation counting Inhibition of IL3 dependent proliferation in C57/B16 mouse bone marrow cells using [3H]thymidine by liquid scintillation counting	[PMID: 24726806]
MV4-11	EC₅₀	10 1 Compound: 1, R406	Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry	[PMID: 24779514]
B-cell	EC₅₀	48 1 Compound: 3, R406	Inhibition of SYK in human B-cells cells assessed as reduction in FcepsilonR1/FcgammaR-mediated signaling responses Inhibition of SYK in human B-cells cells assessed as reduction in FcepsilonR1/FcgammaR-mediated signaling responses	[PMID: 22257213]
HUVEC	EC₅₀	36 1 Compound: 1, R406	Inhibition of KDR in VEGF-stimulated HUVEC assessed as phosphorylation after 1 hr incubation Inhibition of KDR in VEGF-stimulated HUVEC assessed as phosphorylation after 1 hr incubation	[PMID: 24779514]
TF-1	EC₅₀	13 1 Compound: 1, R406	Inhibition of Jak2 in erythropoietin-stimulated human TF1 cells assessed as assessed as phospho-Stat5 after 1 hr incubation Inhibition of Jak2 in erythropoietin-stimulated human TF1 cells assessed as assessed as phospho-Stat5 after 1 hr incubation	[PMID: 24779514]
Bone marrow cell	IC₅₀	147 1 Compound: 2	Inhibition of IL3 dependent proliferation in C57/B16 mouse bone marrow cells using [3H]thymidine by liquid scintillation counting Inhibition of IL3 dependent proliferation in C57/B16 mouse bone marrow cells using [3H]thymidine by liquid scintillation counting	[PMID: 24726806]
MV4-11	EC₅₀	10 1 Compound: 1, R406	Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry	[PMID: 24779514]
HUVEC	EC₅₀	36 1 Compound: 1, R406	Inhibition of KDR in VEGF-stimulated HUVEC assessed as phosphorylation after 1 hr incubation Inhibition of KDR in VEGF-stimulated HUVEC assessed as phosphorylation after 1 hr incubation	[PMID: 24779514]
Ramos	IC₅₀	457 1 Compound: 2	Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay	[PMID: 24726806]
HUVEC	EC₅₀	36 1 Compound: 1, R406	Inhibition of KDR in VEGF-stimulated HUVEC assessed as phosphorylation after 1 hr incubation Inhibition of KDR in VEGF-stimulated HUVEC assessed as phosphorylation after 1 hr incubation	[PMID: 24779514]
Ramos	EC₅₀	53 1 Compound: 1, R406	Inhibition of Syk in antihuman IgM-stimulated human Ramos cells assessed as decrease in BCR-mediated BLNK phosphorylation by cellular assay Inhibition of Syk in antihuman IgM-stimulated human Ramos cells assessed as decrease in BCR-mediated BLNK phosphorylation by cellular assay	[PMID: 24779514]
Ramos	EC₅₀	53 1 Compound: 1, R406	Inhibition of Syk in antihuman IgM-stimulated human Ramos cells assessed as decrease in BCR-mediated BLNK phosphorylation by cellular assay Inhibition of Syk in antihuman IgM-stimulated human Ramos cells assessed as decrease in BCR-mediated BLNK phosphorylation by cellular assay	[PMID: 24779514]
MV4-11	EC₅₀	10 1 Compound: 1, R406	Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry Inhibition of Flt3 in human MV411 cells assessed as assessed as proliferation after 72 hrs incubation by spectrophotometry	[PMID: 24779514]
TF-1	EC₅₀	13 1 Compound: 1, R406	Inhibition of Jak2 in erythropoietin-stimulated human TF1 cells assessed as assessed as phospho-Stat5 after 1 hr incubation Inhibition of Jak2 in erythropoietin-stimulated human TF1 cells assessed as assessed as phospho-Stat5 after 1 hr incubation	[PMID: 24779514]
Ramos	EC₅₀	53 1 Compound: 1, R406	Inhibition of Syk in antihuman IgM-stimulated human Ramos cells assessed as decrease in BCR-mediated BLNK phosphorylation by cellular assay Inhibition of Syk in antihuman IgM-stimulated human Ramos cells assessed as decrease in BCR-mediated BLNK phosphorylation by cellular assay	[PMID: 24779514]
Bone marrow cell	IC₅₀	147 1 Compound: 2	Inhibition of IL3 dependent proliferation in C57/B16 mouse bone marrow cells using [3H]thymidine by liquid scintillation counting Inhibition of IL3 dependent proliferation in C57/B16 mouse bone marrow cells using [3H]thymidine by liquid scintillation counting	[PMID: 24726806]
Ramos	IC₅₀	457 1 Compound: 2	Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay	[PMID: 24726806]
Ramos	IC₅₀	457 1 Compound: 2	Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay	[PMID: 24726806]
SK-N-SH	EC₅₀	80 1 Compound: 3, R406	Inhibition of Ret in human SK-N-SH cells Inhibition of Ret in human SK-N-SH cells	[PMID: 22257213]
TF-1	EC₅₀	13 1 Compound: 1, R406	Inhibition of Jak2 in erythropoietin-stimulated human TF1 cells assessed as assessed as phospho-Stat5 after 1 hr incubation Inhibition of Jak2 in erythropoietin-stimulated human TF1 cells assessed as assessed as phospho-Stat5 after 1 hr incubation	[PMID: 24779514]
THP-1	EC₅₀	171 1 Compound: 3, R406	Inhibition of SYK in human THP1 cells assessed as reduction in FcepsilonR1/FcgammaR-mediated signaling responses Inhibition of SYK in human THP1 cells assessed as reduction in FcepsilonR1/FcgammaR-mediated signaling responses	[PMID: 22257213]

体外実験

R406 inhibits adenosine A3 receptor (IC₅₀=0.081 μM), adenosine transporter (IC₅₀=1.84 μM), and monoamine transporter (IC₅₀=2.74 μM)^[1].
R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC₅₀s of 15.1, 2.9 and 6.3 μM, respectively^[1].
R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	Cultured human mast cells (CHMC)
Concentration:	0.016, 0.08, 0.4, 2 µM
Incubation Time:	40 minutes
Result:	Inhibited all other kinases tested at 5 to 100 fold less potency than Syk as judged by phosphorylation of target proteins.

体内実験

R406 (5 and 10 mg/kg) shows efficacy in the amelioration of the Arthus reaction and in reducing clinical symptoms in the collagen antibody-induced arthritis (CAIA) and K/BxN models of rheumatoid arthritis (RA). Immune complex (IC)-mediated inflammation is reduced by inhibition of Fc receptor signaling with R406^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c mice (6-8 weeks) with CAIA^[1]
Dosage:	5 and 10 mg/kg
Administration:	Administered orally, b.i.d, for 14 days, starting 4 hours after antibody challenge on day 0.
Result:	Reduced inflammation and swelling, and the arthritis progressed more slowly in treated animals than in vehicle controls.

Animal Model:	Female C57BL/6 mice with arthritis^[1]
Dosage:	10 mg/kg
Administration:	Administered orally one hour before serum injection; b.i.d; for 13 days
Result:	Delayed the onset and reduced the severity of clinical arthritis. Paw thickening and clinical arthritis were reduced by approximately 50%.

分子量

470.45

分子式

C₂₂H₂₃FN₆O₅

CAS 番号

841290-80-0

Appearance

Solid

Color

White to light yellow

SMILES

COC1=CC(NC2=NC(NC3=NC(N4)=C(C=C3)OC(C)(C)C4=O)=C(C=N2)F)=CC(OC)=C1OC

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (53.14 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1256 mL	10.6281 mL	21.2562 mL
5 mM	0.4251 mL	2.1256 mL	4.2512 mL
10 mM	0.2126 mL	1.0628 mL	2.1256 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.31 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.07%

Select Batch:

データシート (277 KB) SDS (393 KB)

COA (247 KB) LCMS (107 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. [Content Brief]

[2]. Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1256 mL	10.6281 mL	21.2562 mL	53.1406 mL
	5 mM	0.4251 mL	2.1256 mL	4.2512 mL	10.6281 mL
	10 mM	0.2126 mL	1.0628 mL	2.1256 mL	5.3141 mL
	15 mM	0.1417 mL	0.7085 mL	1.4171 mL	3.5427 mL
	20 mM	0.1063 mL	0.5314 mL	1.0628 mL	2.6570 mL
	25 mM	0.0850 mL	0.4251 mL	0.8502 mL	2.1256 mL
	30 mM	0.0709 mL	0.3543 mL	0.7085 mL	1.7714 mL
	40 mM	0.0531 mL	0.2657 mL	0.5314 mL	1.3285 mL
	50 mM	0.0425 mL	0.2126 mL	0.4251 mL	1.0628 mL

R406 free base Related Classifications

Molarity Calculator
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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

R406841290-80-0R 406R-406SykFLT3ApoptosisSpleen tyrosine kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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R406 free base

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R406 free base 関連抗体

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Complete Stock Solution Preparation Table

R406 free base Related Classifications

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