Fostamatinib disodium hexahydrate (Synonyms: R788 disodium hexahydrate)

Name: Fostamatinib disodium hexahydrate
Brand: MedChemExpress
SKU: HY-13038B
Rating: 5.0 (14 reviews)

Cat. No.: HY-13038B Purity: 99.46%: Data Sheet
COA

SDS
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Fostamatinib (R788) disodium hexahydrate is the oral proagent of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a K_i of 30 nM and an IC₅₀ of 41 nM. R406 also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM).

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

CAS No. : 914295-16-2

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 14 publication(s) in Google Scholar

Other Forms of Fostamatinib disodium hexahydrate:

Fostamatinib Disodium In-stock
Fostamatinib In-stock
Fostamatinib disodium hexahydrate (Standard) Get quote

14 Publications Citing Use of MCE Fostamatinib disodium hexahydrate

Histological Imaging/Staining

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

RT-PCR

: Fostamatinib disodium hexahydrate purchased from MedChemExpress. Usage Cited in: BMC Med. 2024 Mar 5;22(1):96. [Abstract]; CCK-8 assay showed that Fostamatinib (R788, 1.25–20 μM; 5 h) exhibited mild cytotoxicity in a dose-dependent manner.

: Fostamatinib disodium hexahydrate purchased from MedChemExpress. Usage Cited in: BMC Med. 2024 Mar 5;22(1):96. [Abstract]; Western blotting analysis of p-p65, p-IRF3, and p-TBK1 from THP-1 cells subjected to MSA-2 stimulation and treated with Fostamatini (R788, 10–20 μM) or AMX (100–200 μM). The results showed that R788 significantly inhibited the levels of phosphorylated TBK1 (p-TBK1) and IRF3 (p-IRF3), with no effect on p65 phosphorylation (p-p65), indicating the specific inhibition on TBK1 within TBK1/IRF3 signaling pathway.

: Fostamatinib disodium hexahydrate purchased from MedChemExpress. Usage Cited in: BMC Med. 2024 Mar 5;22(1):96. [Abstract]; RT-qPCR showed the relative levels (normalized with GAPDH) of IFNB, TNFA, and IL6 from NSC-34 cells treated with Fostamatinib (R788, 1.25–20 μM).

: Fostamatinib disodium hexahydrate purchased from MedChemExpress. Usage Cited in: Gene. 2020 Jun 20;744:144608. [Abstract]; Cell Counting Kit-8 assay results showing the effect of Fostamatinib (10 μM) on the proliferative capacity of PC-3 cells.

: Fostamatinib disodium hexahydrate purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2014 Aug 22;4(8):e240. [Abstract]; Hematoxylin and eosin-stained liver slides and reticulin stained BM slides are shown from one Fostamatinib (R788, 40 mg/kg; oral gavage; twice daily) treated mouse versus control mouse. Arrows show liver infiltrates in the control group, which are absent in the treatment group. The results showed that in the Fostamatinib (R788, 40 mg/kg; oral gavage; twice daily) group, virtually no infiltration of granulocyte and megakaryocyte progenitor cells was observed in the liver.

: Fostamatinib disodium hexahydrate purchased from MedChemExpress. Usage Cited in: Blood Cancer J. 2014 Aug 22;4(8):e240. [Abstract]; Fostamatinib (R788, 40 mg/kg; oral gavage; twice a day) significantly improved the survival rate of Balb/c mice transplanted with the TEL‑SYK oncogene by inhibiting SYK (Fig. a), effectively reduced the sizes of the spleen and liver (Fig. b), and decreased white blood cell (WBC) counts simultaneously (Fig. c).

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Description

Fostamatinib (R788) disodium hexahydrate is the oral proagent of the active compound R406^[1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a K_i of 30 nM and an IC₅₀ of 41 nM^[2]. R406 also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM)^[3].

IC₅₀ & Target

Syk, FLT3^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
Ramos	IC₅₀	0.267 μM Compound: 1	Cytotoxicity against human Ramos cells Cytotoxicity against human Ramos cells	[PMID: 23151054]

In Vivo

Fostamatinib (R788) is highly bioavailable, and rapidly absorbed in Louvain rats. R406 following a single oral dose of R788 10 mg/kg or 20 mg/kg: AUC_{0-16 hrs}= 10618 ng*h/mL and 30650 ng*h/mL respectively; C_max=2600 ng/mL and 6500 ng/mL respectively (observed at 1 hour); t_1/2=4.2 hours. The prodrug was not detected in plasma suggesting R788 is completely converted to R406^[1].

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

Molecular Weight

732.51

Formula

C₂₃H₃₆FN₆Na₂O₁₅P

CAS No.

914295-16-2

Appearance

Solid

Color

White to gray

SMILES

COC1=CC(NC2=NC=C(C(NC3=NC(N4COP(O[Na])(O[Na])=O)=C(C=C3)OC(C)(C)C4=O)=N2)F)=CC(OC)=C1OC.O.O.O.O.O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (34.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2 mg/mL (2.73 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3652 mL	6.8258 mL	13.6517 mL
5 mM	0.2730 mL	1.3652 mL	2.7303 mL
10 mM	0.1365 mL	0.6826 mL	1.3652 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% CMC-Na/saline water
Solubility: 8.33 mg/mL (11.37 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.46%

Select Batch:

Data Sheet (278 KB) SDS (394 KB)

COA (256 KB) HNMR (151 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36(4):273. [Content Brief]

[2]. 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]

[3]. 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

H₂O / DMSO	1 mM	1.3652 mL	6.8258 mL	13.6517 mL	34.1292 mL
DMSO	5 mM	0.2730 mL	1.3652 mL	2.7303 mL	6.8258 mL
	10 mM	0.1365 mL	0.6826 mL	1.3652 mL	3.4129 mL
	15 mM	0.0910 mL	0.4551 mL	0.9101 mL	2.2753 mL
	20 mM	0.0683 mL	0.3413 mL	0.6826 mL	1.7065 mL
	25 mM	0.0546 mL	0.2730 mL	0.5461 mL	1.3652 mL
	30 mM	0.0455 mL	0.2275 mL	0.4551 mL	1.1376 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Fostamatinib disodium hexahydrate Related Classifications

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:

Fostamatinib disodium hexahydrate914295-16-2R788 disodium hexahydrateSykFLT3Spleen tyrosine kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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Fostamatinib disodium hexahydrate (Synonyms: R788 disodium hexahydrate)

Customer Review

Other Forms of Fostamatinib disodium hexahydrate:

Fostamatinib disodium hexahydrate Related Antibodies

14 Publications Citing Use of MCE Fostamatinib disodium hexahydrate

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•Related Screening Libraries:

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•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

Fostamatinib disodium hexahydrate Related Classifications

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