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Fostamatinib (R788) disodium

別名: Tamatinib Fosdium 中文名稱：福他替尼二鈉鹽

Fostamatinib disodium (R788, Tamatinib Fosdium)是活性代謝物R406的前體藥物，是一種Syk抑制劑，無細(xì)胞試驗(yàn)中IC50為41 nM，強(qiáng)效抑制Syk但不抑制Lyn，對(duì)Flt3作用效果弱5倍。Phase 3。

Fostamatinib (R788) disodium Chemical Structure

Fostamatinib (R788) disodium Chemical Structure

CAS: 1025687-58-4

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
5mg 1374.44 現(xiàn)貨
10mg 2603.72 現(xiàn)貨
50mg 7953.61 現(xiàn)貨
250mg 13677.3 現(xiàn)貨
1g 32678.1 現(xiàn)貨
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Fostamatinib (R788) disodium相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Syk Signaling Pathways

Syk信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
Ramos Function assay Inhibition of SYK in human Ramos cells, IC50 = 0.267 μM. 23350847
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
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生物活性

產(chǎn)品描述 Fostamatinib disodium (R788, Tamatinib Fosdium)是活性代謝物R406的前體藥物，是一種Syk抑制劑，無細(xì)胞試驗(yàn)中IC50為41 nM，強(qiáng)效抑制Syk但不抑制Lyn，對(duì)Flt3作用效果弱5倍。Phase 3。
特性 R935788是臨床上常用的藥物前體 R406的口服試劑, 在藥物性能上優(yōu)于R406，具有較高的溶解度和生物利用度。
靶點(diǎn)
Syk [1]
(Cell-free assay)
41 nM
體外研究(In Vitro)
體外研究活性 R935788是R406亞甲基磷酸言藥物前體,可在體內(nèi)快速轉(zhuǎn)化為R406。R406(R935788的活性形式)選擇性抑制Syk依賴性信號(hào)，EC50為33 nM 到171 nM,比作用于Syk非依賴性通路更有效。[1] R406抑制多種彌散性大B細(xì)胞淋巴瘤(DLBCL)細(xì)胞系增殖，EC50為 0.8 μM到8.1 μM。[2] R406 處理，降低BLNK, Akt, GSK-3, FOXO和ERK 磷酸化。此外, R406作用于TCL1白血病，完全抑制抗-IgM抗體誘導(dǎo)的BCR信號(hào)。盡管TCL1白血病中存在高水平的組成型激活的Syk，但是R406對(duì)白血病細(xì)胞沒有選擇毒性。[3]
激酶實(shí)驗(yàn) 體外熒光偏振激酶檢測(cè)實(shí)驗(yàn)
R406在 DMSO中連續(xù)稀釋，然后在激酶buffer(20 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM MnCl2, 1 mM DTT, 0.1 mg/mL 乙酰 BGG)中稀釋到 1% DMSO。室溫下，在激酶 buffer中加入ATP和底物，使DMSO 終濃度為0.2%。在含 5 μM HS1 肽底物和 4 μM ATP 的混合物中進(jìn)行激酶反應(yīng)，終體積為 20 μL，然后在激酶buffer中加入0.125 ng Syk 開始反應(yīng)。反應(yīng)在室溫下進(jìn)行40分鐘。加入含EDTA/抗磷酸抗體/熒光磷酸示蹤物（在FP 稀釋 Buffer中稀釋）的20 μL PTK淬滅混合物，反應(yīng)終止。反應(yīng)在室溫下暗中反應(yīng)30分鐘，然后在Polarion 熒光偏振酶標(biāo)儀上讀數(shù)。通過與酪氨酸激酶實(shí)驗(yàn)試劑盒中的磷酸競(jìng)爭(zhēng)劑競(jìng)爭(zhēng)獲得校準(zhǔn)曲線，數(shù)據(jù)轉(zhuǎn)換為磷酸數(shù)量。為了測(cè)定IC50，測(cè)定11種濃度R406，重復(fù)進(jìn)行實(shí)驗(yàn)，使用 Prism GraphPad 軟件，通過非線性回歸分析進(jìn)行曲線擬合。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 TCL1-002, TCL1-252, TCL1-551, TCL1-870, 和TCL1-540
濃度 溶于DMSO,終濃度為~10 μM
孵育時(shí)間 48小時(shí)
方法

使用濃度不斷增高的R406處理細(xì)胞 48小時(shí)。使用碘化丙啶(PI)和膜聯(lián)蛋白-A5–FITC 聯(lián)合雙染色，測(cè)定凋亡細(xì)胞百分?jǐn)?shù)。使用 FITC小鼠抗–Ki-67 抗體進(jìn)行 Ki-67染色。通過FACSCalibur流式細(xì)胞儀，使用CellQuest Version 3.3 軟件分析樣本。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot p-JAK2 / JAK2 / p-SRC / SRC / p-FAK / FAK / p-SYK / SYK / p-ERK / ERK p-SYK(525-526) / t-SYK / p-SYK(323) / p-BTK / t-BTK p-MEK / MEK / p-ERK / ERK / p-AKT / AKT 29340070
Growth inhibition assay Cell viability 25748087
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 考慮到R406作用于小鼠的血漿半衰期短于 2小時(shí)，R935788分3次給藥，每次間隔3小時(shí)，確保在每次給藥期間Syk得到持續(xù)抑制，模仿作用于人類的較長(zhǎng)血漿半衰期 (15小時(shí))。盡管在體外細(xì)胞毒性作用相對(duì)溫和，但是R935788在體內(nèi)顯著抑制白血病細(xì)胞增殖和存活，這與阻止抗原依賴性B細(xì)胞受體（BCR）的信號(hào)相關(guān)，而與抑制組成型Syk活性無關(guān)。R935788每天按80 mg/kg劑量處理小鼠，持續(xù) 18-21 天，有效抑制 TCL1-002, TCL1-551 和 TCL1-870腫瘤生長(zhǎng)，在處理末期觀察不到白血病 CD5+/B220+細(xì)胞，R935788顯著延長(zhǎng)處理鼠的壽命，平均壽命從 45/46天提高到170/172 天, 且在后期6個(gè)月的處理期間完全根除相當(dāng)大比例的惡性細(xì)胞，且不會(huì)影響正常 B 淋巴細(xì)胞的產(chǎn)生。R935788治療也誘導(dǎo)正常和惡性B細(xì)胞從脾臟和淋巴結(jié)中短暫遷移到外周血中，隨后選擇性抑制惡性B細(xì)胞生長(zhǎng)。此外, R935788作用于Eμ-TCL1轉(zhuǎn)基因小鼠，也有效作用于自發(fā)的TCL1白血病。[3]
動(dòng)物實(shí)驗(yàn) Animal Models 腹腔注射 TCL1-002, TCL1-551, 或 TCL1-870 白血病細(xì)胞的雌性B6/C3H F1小鼠 , 和 Eμ-TCL1轉(zhuǎn)基因小鼠
Dosages 80 mg/kg/day
Administration 分3種劑量每個(gè)3小時(shí)腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05904093 Not yet recruiting
Sickle Cell Disease|Hb-SS Disease|Hemoglobin S|Disease Sickle Cell Anemia|Sickle Cell Disorders|Hemoglobin Beta Thalassemia Disease
National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 1
NCT05509582 Enrolling by invitation
Immune Mediated Anemia|Immune Mediated Thrombocytopenia|Chronic GVHD
National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 2
NCT06071520 Completed
Primary Immune Thrombocytopenia
Fundación Pública Andaluza para la gestión de la Investigación en Sevilla
 March 1 2023 --
NCT05613296 Not yet recruiting
ITP - Immune Thrombocytopenia|Chronic ITP|Refractory ITP
Gruppo Italiano Malattie EMatologiche dell''Adulto
 February 2023 --
NCT04543279 Terminated
Myelofibrosis|Thrombocytopenia
Washington University School of Medicine|Rigel Pharmaceuticals
 May 3 2021 Phase 2
NCT04904276 Terminated
ITP|Immune Thrombocytopenia
Rigel Pharmaceuticals
 May 18 2021 --

化學(xué)信息&溶解度

分子量 624.42 分子式

C23H24FN6O9P.2Na
CAS號(hào) 1025687-58-4 SDF Download Fostamatinib (R788) disodium SDF
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.[Na+].[Na+]
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 12 mg/mL ( (19.21 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 1:
What’s the difference between S2625 and S2206?

回答：
The differences between S2625 and S2206: 1. S2206 is more stable than S2625; 2. The water solubility of S2206 is better than S2625; 3. The absorption of S2206 is harder than S2625, so you need to test the suitable dosage if you use the product in animal assays; 4. The potency of S2206 and S2625 is similar.

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