Fostamatinib (R788) disodium

別名: Tamatinib Fosdium 中文名稱：福他替尼二鈉鹽

目錄號：S2206 Purity: 99.99%

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

Fostamatinib (R788) disodium Chemical Structure

CAS: 1025687-58-4

規(guī)格	價格	庫存
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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產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

Fostamatinib (R788) disodium相關(guān)產(chǎn)品

相關(guān)靶點	ZAP70	點擊展開
相關(guān)產(chǎn)品	R406 R406 (free base) PRT062607 (P505-15) HCl Entospletinib (GS-9973) Piceatannol BAY-61-3606 PRT-060318 2HCl TAK-659 Hydrochloride RO9021	點擊展開
相關(guān)化合物庫	酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫血管生成相關(guān)化合物庫 HIF-1信號通路化合物庫 FDA抗癌藥物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	活性描述	文獻信息
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

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

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，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細胞淋巴瘤(DLBCL)細胞系增殖，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抗體誘導的BCR信號。盡管TCL1白血病中存在高水平的組成型激活的Syk，但是R406對白血病細胞沒有選擇毒性。^[3]
激酶實驗	體外熒光偏振激酶檢測實驗
激酶實驗	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 的混合物中進行激酶反應，終體積為 20 μL，然后在激酶buffer中加入0.125 ng Syk 開始反應。反應在室溫下進行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，反應終止。反應在室溫下暗中反應30分鐘，然后在Polarion 熒光偏振酶標儀上讀數(shù)。通過與酪氨酸激酶實驗試劑盒中的磷酸競爭劑競爭獲得校準曲線，數(shù)據(jù)轉(zhuǎn)換為磷酸數(shù)量。為了測定IC50，測定11種濃度R406，重復進行實驗，使用 Prism GraphPad 軟件，通過非線性回歸分析進行曲線擬合。
細胞實驗	細胞系	TCL1-002, TCL1-252, TCL1-551, TCL1-870, 和TCL1-540
	濃度	溶于DMSO,終濃度為~10 μM
	孵育時間	48小時
	方法	使用濃度不斷增高的R406處理細胞 48小時。使用碘化丙啶(PI)和膜聯(lián)蛋白-A5–FITC 聯(lián)合雙染色，測定凋亡細胞百分數(shù)。使用 FITC小鼠抗–Ki-67 抗體進行 Ki-67染色。通過FACSCalibur流式細胞儀，使用CellQuest Version 3.3 軟件分析樣本。
實驗圖片	檢測方法	檢測指標	實驗圖片	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，R935788分3次給藥，每次間隔3小時，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血漿半衰期 (15小時)。盡管在體外細胞毒性作用相對溫和，但是R935788在體內(nèi)顯著抑制白血病細胞增殖和存活，這與阻止抗原依賴性B細胞受體（BCR）的信號相關(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，在處理末期觀察不到白血病 CD5⁺/B220⁺細胞，R935788顯著延長處理鼠的壽命，平均壽命從 45/46天提高到170/172 天, 且在后期6個月的處理期間完全根除相當大比例的惡性細胞，且不會影響正常 B 淋巴細胞的產(chǎn)生。R935788治療也誘導正常和惡性B細胞從脾臟和淋巴結(jié)中短暫遷移到外周血中，隨后選擇性抑制惡性B細胞生長。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]
動物實驗	Animal Models	腹腔注射 TCL1-002, TCL1-551, 或 TCL1-870 白血病細胞的雌性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3小時腹腔注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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	--

參考文獻
[1] Braselmann S, et al. J Pharmacol Exp Ther, 2006, 319(3), 998-1008. [2] Chen L, et al. Blood, 2008, 111(4), 2230-2237. [3] Suljagic M, et al. Blood, 2010, 116(23), 4894-4905.

參考文獻

[1] Braselmann S, et al. J Pharmacol Exp Ther, 2006, 319(3), 998-1008.
[2] Chen L, et al. Blood, 2008, 111(4), 2230-2237.
[3] Suljagic M, et al. Blood, 2010, 116(23), 4894-4905.

化學信息&溶解度

分子量	624.42	分子式	C₂₃H₂₄FN₆O₉P.2Na
CAS號	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+]
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

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

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (160.14 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 3 mg/mL (4.8 mM)

Ethanol : Insoluble

Water : 12 mg/mL (19.21 mM)

DMSO : Insoluble ( ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : Insoluble

5%TFA : 4.25 mg/mL (6.8 mM)

DMSO : 0.4 mg/mL ( (0.64 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

DMSO : 100 mg/mL ( (160.14 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 13 mg/mL (20.81 mM)

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

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

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(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，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Fostamatinib (R788) disodium

產(chǎn)品質(zhì)控

Fostamatinib (R788) disodium相關(guān)產(chǎn)品

相關(guān)信號通路圖

細胞實驗數(shù)據(jù)示例

生物活性

化學信息&溶解度

實驗計算

技術(shù)支持

常見問題及建議解決方法