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  1. Cell Cycle/DNA Damage Cytoskeleton
  2. PAK
  3. FRAX597

FRAX597 是一種有效的 I型 P21激活激酶 (PAK)抑制劑,作用于 PAK1,23IC50 分別為 8,13 和 19 nM。

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FRAX597 Chemical Structure

FRAX597 Chemical Structure

CAS No. : 1286739-19-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥1044
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2 mg ¥400
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5 mg ¥850
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10 mg ¥1400
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50 mg ¥3600
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100 mg ¥5200
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

查看 PAK 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.

IC50 & Target[1]

PAK1

8 nM (IC50)

PAK2

13 nM (IC50)

PAK3

19 nM (IC50)

體外研究
(In Vitro)

FRAX597 is determined to be a potent, ATP-competitive inhibitor of group I PAKs (PAK 1-3), with biochemical IC50 values as follows: PAK1 IC50=8 nM, PAK2 IC50=13 nM, PAK3 IC50=19 nM. The IC50 toward PAK4, a member of group II PAKs is >10 μM. At a concentration of 100 nM FRAX597 displays a significant (>80% inhibition) inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%). When measured using the Kinase Glo Assay in the presence of 20 nM protein and 1 μM ATP, FRAX597 displayed an IC50 value of 48 nM against wild type PAK1, while IC50 values against the V342F and V342Y PAK1 mutants are higher than 3 μM and 2 μM, respectively[1].

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

體內(nèi)研究
(In Vivo)

Analysis of the flux reading for the animals in the two cohorts demonstrates a significantly slower tumor growth rate in FRAX597-treated mice compared with control mice. After 14 days of treatment the animals are sacrificed and the tumors excised and weighed. FRAX597-treated cohort shows significantly lower average tumor weight compared with the control cohort [1].

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

分子量

558.10

Formula

C29H28ClN7OS

CAS 號(hào)
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 14.29 mg/mL (25.60 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.7918 mL 8.9590 mL 17.9179 mL
5 mM 0.3584 mL 1.7918 mL 3.5836 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 1.43 mg/mL (2.56 mM); 懸濁液; 超聲助溶

    此方案可獲得 1.43 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

    1 mL 工作液為例,取 100 μL 14.3 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 1.43 mg/mL (2.56 mM); 懸濁液; 超聲助溶

    此方案可獲得 1.43 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

    1 mL 工作液為例,取 100 μL 14.3 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。

掃碼獲得
動(dòng)物溶解方案

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO PEG300/PEG400Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
純度 & 產(chǎn)品資料

純度: 99.36%

參考文獻(xiàn)
Cell Assay
[1]

30,000 SC4 cells/well are plated in 12-well dishes in triplicate. Cell growth media with or without FRAX597 (1 μM) is replaced daily. At indicated time points, cells from individual wells are trypsinized and counted using a Coulter counter. Statistical analysis is performed using a Student's t test. For cell cycle analysis, cells are harvested, washed once with PBS and fixed in cold 70% ethanol. Fixed cells are resuspended in propidium iodide (PI) buffer (50 μg/mL PI, 250 mg/mL RNase A in PBS) and incubated overnight at 4°C in the dark. Cell cycle distribution is evaluated using Coulter Epics XL flow cytometer. Data are analyzed using WinMDI software[1].

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

Animal Administration
[1]

Mice[1]
Nf2-/- SC4 Schwann cells are transduced by lentiviruses carrying pLuc-mCherry and sorted by FACS. 5×104 cells are transplanted into the sciatic nerve sheath of NOD/SCID mice (8 weeks of age) by intraneural injection. Tumor progression is monitored weekly by bioluminescence imaging (BLI) on an IVIS-200 system. The representative images from bioluminescence imaging (BLI) of mice carrying orthotopic tumors treated with FRAX597 (100 mg/kg) or vehicle control at day 14 of treatment. NOD/SCID mice are injected intraneurally with 5×104 SC4/pLuc-mCherry cells and are enrolled into treatment after 10 days. Mice are treated daily for 14 days and imaged every 3 days to follow tumor development.

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

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7918 mL 8.9590 mL 17.9179 mL 44.7948 mL
5 mM 0.3584 mL 1.7918 mL 3.5836 mL 8.9590 mL
10 mM 0.1792 mL 0.8959 mL 1.7918 mL 4.4795 mL
15 mM 0.1195 mL 0.5973 mL 1.1945 mL 2.9863 mL
20 mM 0.0896 mL 0.4479 mL 0.8959 mL 2.2397 mL
25 mM 0.0717 mL 0.3584 mL 0.7167 mL 1.7918 mL

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產(chǎn)品名稱:
FRAX597
目錄號(hào):
HY-15542A
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