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R406 R406 is a potent inhibitor of immunoglobulin E (IgE)- and IgG-mediated activation of Fc receptor signaling (EC(50) for degranulation=56-64 nM). The primary target for R406 is the spleen tyrosine kinase (Syk). R406 inhibited phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. R406 bound to the ATP binding pocket of Syk and inhibited its kinase activity as an ATP-competitive inhibitor (K(I)=30 nM). Furthermore, R406 blocked Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and BCR-mediated activation of B lymphocytes. R406 is orally bioavailable, achieving exposures capable of inhibiting Syk-dependent IgE-mediated basophil activation. Collectively, the results show R406 potential for modulating Syk activity in human disease. Synonyms: R 406; R-406. CAS No. 841290-80-0. Molecular formula: C22H23FN6O5. Mole weight: 470.45. BOC Sciences 9
R406 Benzenesulfonate R406 is a potent Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Synonyms: R406; R 406; R-406. Grades: >98%. CAS No. 841290-81-1. Molecular formula: C28H29FN6O8S. Mole weight: 628.63. BOC Sciences 9
Syk Inhibitor VI, R406 (N4-(2,2-Dimethyl-3-oxo-4H-pyrid[1,4]oxazin-6-yl)-5-fluoro-N2-(3,4,5-trimethoxyphenyl)-2,4-pyrimidinediamine, 6- (5-Fluoro-2- (3, 4, 5-trimethoxyphenylamino) pyrimidin-4-ylamino) -2, 2-dimethyl-2H-pyrido[3, 2-b][1, 4]oxazin-3 (4H) -one) A cell-permeable, orally bioavailable pyrimidinediamino compound with anti-inflammatory and anti-tumor properties. Acts as a potent, reversible and ATP-competitive inhibitor of Syk kinase (IC50 = 41nM; Ki = 30nM). Exhibits high selectivity over a broad panel of other protein kinases (˜300nM), ion channels, and enzymes. Blocks Syk-dependent FcR-mediated activation of monocytes/macrophages, and neutrophils and inhibits Anti-IgE-mediated degranulation in cultured human mast cells (EC50 = 56nM as measured by tryptase release). At higher concentrations, it is shown to block adenosine A3 receptors, adenosine transporter, and monoamine transporter (IC50 = 81nM, 1.84uM, and 2.74uM, respectively), and Flt3 autophosphorylation. Shown to reduce immune complex-mediated inflammation in murine models (˜10mg/kg) and diminish airway hyper-responsiveness in asthma models. Group: Biochemicals. Grades: Highly Purified. CAS No. 841290-80-0. Pack Sizes: 5mg. US Biological Life Sciences. USBiological 4
Worldwide
Annonacin Annonacin is an acetylgenin that is toxic by inhibiting the pathway of the mitochondrial complex. Annonacin increases tau phosphorylation in R406W +/+ mice. Annonacin acts as an inhibitor of the sodium/potassium and sarcoplasmic reticulum (SERCA) ATPase pumps. Annonacin has significant killing effect on ovarian cancer cell, cervical cancer cell, breast cancer cell, bladder cancer cell and skin cancer cell. Annonacin induces apoptosis through Bax and Caspase-3-related pathways [1] [2] [3] [4]. Uses: Scientific research. Group: Natural products. CAS No. 111035-65-5. Pack Sizes: 1 mg. Product ID: HY-N2877. MedChemExpress MCE
Fostamatinib Fostamatinib, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibiting Syk but not Lyn, and 5-fold less potent to Flt3. Synonyms: R788; R 788; R-788. Grades: >98%. CAS No. 901119-35-5. Molecular formula: C23H26FN6O9P. Mole weight: 580.46. BOC Sciences 10
Fostamatinib Fostamatinib (R788) 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 IC 50 of 41 nM [2]. R406 also inhibits Lyn (IC 50 =63 nM) and Lck (IC 50 =37 nM) [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: R788. CAS No. 901119-35-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13038A. MedChemExpress MCE
Fostamatinib Disodium Fostamatinib Disodium (R788 Disodium) 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 IC 50 of 41 nM [2]. R406 also inhibits Lyn (IC 50 =63 nM) and Lck (IC 50 =37 nM) [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: R788(Disodium). CAS No. 1025687-58-4. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13038. MedChemExpress MCE
Fostamatinib sodium R788 (Fostamatinib) disodium, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3. Synonyms: R935788. Code names: R788 sodium. R935788 sodium. CAS No. 1025687-58-4. Molecular formula: C23H24FN6O9P.2Na. Mole weight: 624.42. BOC Sciences 10
R788 disodium hexahydrate R788 sodium salt hydrate, a methylene phosphate prodrug of the active metabolite R406, is a potent Syk inhibitor. It can be rapidly converted to R406 in vivo. It 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. Synonyms: Fostamatinib disodium hexahydrate; R788 disodium hexahydrate; R 788 disodium hexahydrate; R-788 disodium hexahydrate. Grades: >98%. CAS No. 914295-16-2. Molecular formula: C23H24FN6Na2O9P. Mole weight: 624.42. BOC Sciences 9

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