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R788 disodium hexahydrate

CAS# 914295-16-2

R788 disodium hexahydrate

Catalog No. BCC5127----Order now to get a substantial discount!

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R788 disodium hexahydrate: 5mg $138 In Stock
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Chemical structure

R788 disodium hexahydrate

3D structure

Chemical Properties of R788 disodium hexahydrate

Cas No. 914295-16-2 SDF Download SDF
PubChem ID 24828759 Appearance Powder
Formula C23H24FN6Na2O9P M.Wt 624.42
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Fostamatinib disodium hexahydrate
Solubility DMSO : 31.81 mg/mL (43.43 mM; Need ultrasonic)
H2O : 2 mg/mL (2.73 mM; ultrasonic and warming and heat to 60°C)
Chemical Name disodium;[6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl phosphate;hexahydrate
SMILES CC1(C(=O)N(C2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)COP(=O)([O-])[O-])C.O.O.O.O.O.O.[Na+].[Na+]
Standard InChIKey ZQGJCHHKJNSPMS-UHFFFAOYSA-L
Standard InChI InChI=1S/C23H26FN6O9P.2Na.6H2O/c1-23(2)21(31)30(11-38-40(32,33)34)20-14(39-23)6-7-17(28-20)27-19-13(24)10-25-22(29-19)26-12-8-15(35-3)18(37-5)16(9-12)36-4;;;;;;;;/h6-10H,11H2,1-5H3,(H2,32,33,34)(H2,25,26,27,28,29);;;6*1H2/q;2*+1;;;;;;/p-2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of R788 disodium hexahydrate

DescriptionR788 sodium salt hydrate (Fostamatinib), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM. IC50 Value: 41 nM [1] Target: Syk in vitro: R788 is a methylene phosphate prodrug of R406, which can be rapidly converted to R406 in vivo. R406 (in vitro active form of R788) selectively inhibits Syk-dependent signaling with EC50 values ranging from 33 nM to 171 nM, more potently than Syk-independent pathways in different cells [1]. R406 inhibits cellular proliferation of a variety of diffuse large B-cell lymphoma (DLBCL) cell lines with EC50 values ranging from 0.8 μM to 8.1 μM [2]. R406 treatment reduces basal phosphorylation of BLNK, Akt, glycogen synthase kinase-3 (GSK-3), forkhead box O (FOXO) and ERK not only in cells with high (TCL-002) but also in cells with low levels of phosphorylated Syk (TCL1-551). In addition, R406 completely inhibits the anti-IgM induced Bcr signal in TCL1 leukemias. Despite the higher levels of constitutively active Syk in TCL1 leukemias, R406 is not selectively cytotoxic to the leukemic cells [3]. in vivo: R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals [3].

References:
[1]. Braselmann, S., 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. 319(3): p. 998-1008. [2]. Chen, L., et al., SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood, 2008. 111(4): p. 2230-7. [3]. Suljagic, M., et al., The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the Emu- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. Blood, 2010. 116(23): p. 4894-905.

R788 disodium hexahydrate Dilution Calculator

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R788 disodium hexahydrate Molarity Calculator

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Preparing Stock Solutions of R788 disodium hexahydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.6015 mL 8.0074 mL 16.0149 mL 32.0297 mL 40.0372 mL
5 mM 0.3203 mL 1.6015 mL 3.203 mL 6.4059 mL 8.0074 mL
10 mM 0.1601 mL 0.8007 mL 1.6015 mL 3.203 mL 4.0037 mL
50 mM 0.032 mL 0.1601 mL 0.3203 mL 0.6406 mL 0.8007 mL
100 mM 0.016 mL 0.0801 mL 0.1601 mL 0.3203 mL 0.4004 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on R788 disodium hexahydrate

R788 sodium salt hydrate (Fostamatinib), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.

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Description

Fostamatinib disodium hexahydrate (R788 disodium hexahydrate), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.

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