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  2. MAPK/ERK Pathway
  3. Raf
  4. SB-590885

SB-590885 是一種有效的 B-Raf 抑制劑，Ki 值為 0.16 nM；對(duì)其選擇性是對(duì) c-Raf 的 11 倍多。

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SB-590885 Chemical Structure

SB-590885 Chemical Structure

CAS No. : 405554-55-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1326
In-stock
5 mg ￥753
In-stock
10 mg ￥1205
In-stock
50 mg ￥4750
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100 mg 現(xiàn)貨 詢(xún)價(jià)
200 mg   詢(xún)價(jià)  
500 mg   詢(xún)價(jià)  

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查看 Raf 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

SB-590885 is a potent?B-Raf?inhibitor with?Ki?of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.

IC50 & Target[1]

B-Raf

0.16 nM (Ki)

c-Raf

1.72 nM (Ki)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
370 nM
Compound: 2; SB-590885
Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 48 hrs by CellTiter-Glo assay
[PMID: 29461827]
A549 EC50
0.028 μM
Compound: 6, SB-590885
Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human A549 cells after 60 mins by Western blot analysis
Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human A549 cells after 60 mins by Western blot analysis
[PMID: 22222036]
COLO 205 EC50
0.028 μM
Compound: 6, SB-590885
Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human Colo205 cells after 60 mins by Western blot analysis
Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human Colo205 cells after 60 mins by Western blot analysis
[PMID: 22222036]
HCT-116 EC50
1.1 μM
Compound: 6, SB-590885
Growth inhibition of human HCT116 cells expressing wild-type B-Raf and K-Ras2 G13D mutant after 72 hrs by WST-1 assay
Growth inhibition of human HCT116 cells expressing wild-type B-Raf and K-Ras2 G13D mutant after 72 hrs by WST-1 assay
[PMID: 22222036]
HFF EC50
1.1 μM
Compound: 6, SB-590885
Inhibition of B-Raf-mediated Erk phosphorylation in human HFF cells after 60 mins by Western blot analysis
Inhibition of B-Raf-mediated Erk phosphorylation in human HFF cells after 60 mins by Western blot analysis
[PMID: 22222036]
HMEC EC50
1.1 μM
Compound: 6, SB-590885
Inhibition of B-Raf-mediated Erk phosphorylation in human HMEC cells after 60 mins by Western blot analysis
Inhibition of B-Raf-mediated Erk phosphorylation in human HMEC cells after 60 mins by Western blot analysis
[PMID: 22222036]
HT-29 EC50
0.028 μM
Compound: 6, SB-590885
Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human HT-29 cells after 60 mins by Western blot analysis
Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human HT-29 cells after 60 mins by Western blot analysis
[PMID: 22222036]
PrEC EC50
1.1 μM
Compound: 6, SB-590885
Inhibition of B-Raf-mediated Erk phosphorylation in human PREC cells after 60 mins by Western blot analysis
Inhibition of B-Raf-mediated Erk phosphorylation in human PREC cells after 60 mins by Western blot analysis
[PMID: 22222036]
SK-MEL-2 EC50
1.1 μM
Compound: 6, SB-590885
Growth inhibition of human SK-MEL-2 cells expressing wild-type B-Raf and N-Ras2 Q61R mutant after 72 hrs by WST-1 assay
Growth inhibition of human SK-MEL-2 cells expressing wild-type B-Raf and N-Ras2 Q61R mutant after 72 hrs by WST-1 assay
[PMID: 22222036]
體外研究
(In Vitro)

SB-590885 對(duì) B-Raf 顯示出顯著的選擇性，而對(duì) c-Raf 的 Ki 值為 0.16 nM 而非 1.72 nM。SB-590885 是一種比之前描述的 Raf/VEGFR 激酶抑制劑 BAY 439006（突變型 B-Raf 的 Ki=38 nM，c-Raf 的 Ki=6 nM）更有效的抑制劑。SB-590885 對(duì) 46 種其他激酶顯示出強(qiáng)大的選擇性。與多激酶抑制劑 BAY43-9006 不同，SB-590885 可穩(wěn)定活性構(gòu)型中的致癌 B-Raf 激酶域。在表達(dá)致癌 B-RafV600E 的 Colo205、HT29、A375P、SKMEL28 和 MALME-3M 細(xì)胞中，SB-590885 處理可有效抑制 ERK 磷酸化，EC50 值分別為 28 nM、58 nM、290 nM、58 nM 和 190 nM，并持續(xù)抑制增殖，EC50 值分別為 0.1 μM、0.87 μM、0.37 μM、0.12 μM 和 0.15 μM。 SB-590885 以 BRAF 突變選擇性方式降低黑色素瘤細(xì)胞系的錨定非依賴(lài)性生長(zhǎng)[1]。SB-590885 對(duì) B-Raf 表現(xiàn)出高親和力，Kd 值為 0.3 nM[2]。大多數(shù)攜帶 BRAF V600E 突變且缺乏 CDK4 突變（451Lu、WM35 和 WM983）的黑色素瘤細(xì)胞系對(duì) SB-590885 高度敏感，IC50 值為 <1 μM?；蚪M擴(kuò)增導(dǎo)致的細(xì)胞周期蛋白 D1 水平升高會(huì)介導(dǎo) B-Raf V600E 突變黑色素瘤對(duì) SB-590885 產(chǎn)生耐藥性[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

SB-590885 的給藥可有效降低由表達(dá) B-Raf 的突變型 A375P 黑色素瘤細(xì)胞建立的小鼠異種移植中的腫瘤發(fā)生，并輕度抑制腫瘤生長(zhǎng)[1]。

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

453.54

Formula

C27H27N5O2
CAS 號(hào)
性狀

固體

顏色

White 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 : 10 mg/mL (22.05 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)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 2.2049 mL 11.0244 mL 22.0488 mL
5 mM 0.4410 mL 2.2049 mL 4.4098 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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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: ≥ 2.5 mg/mL (5.51 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.51 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 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。
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

只
由于實(shí)驗(yàn)過(guò)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(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.77%

參考文獻(xiàn)
Cell Assay
[1]

For proliferation assays, cells are treated with compounds in 0.1% DMSO and incubated for 72 hours at 37°C, 5% CO2. Viable cells are quantified using CellTiter-Glo reagent and luminescence detection on a Victor 2V plate reader. Cells are prepared for cell cycle analysis on a Becton Dickinson FACScan, according to the manufacturer's instructions. Data is acquired and analyzed using CellQuest v3.3 software. Anchorage-independent growth assays are done as described elsewhere, with inhibitors or DMSO vehicle included in the agar layer. Cultures are re-fed with media and inhibitor or DMSO every 5 to 7 days for a total of 28 days. Colonies are visualized and photographed by conventional light microscopy and quantified by counting on a grid in triplicate.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

The pharmacokinetic properties and safety of SB-590885, following i.p. injection, are determined and 50 mg/kg daily injections are found to give therapeutic levels with minimal body weight changes. Tumors are initiated in 8- to 12-week-old female nude mice by s.c. injection of 5×106?A375P cells in Matrigel suspension, and 3 weeks after tumor induction when the tumors had reached a volume of 150 to 250 mm3, mice are randomized into groups of eight prior to treatment. Animals are treated with vehicle [2%?N,N-dimethylacetamide, 2% Cremophor EL, and 96% acidified water (pH 4-5)], or vehicle containing 50 mg/kg of SB-590885 daily for 21 days. A cohort of mice treated with SB-590885 are then observed an additional 14 days following cessation of treatment. Tumor volume is measured for 55 days by calipers twice weekly.

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 2.2049 mL 11.0244 mL 22.0488 mL 55.1219 mL
5 mM 0.4410 mL 2.2049 mL 4.4098 mL 11.0244 mL
10 mM 0.2205 mL 1.1024 mL 2.2049 mL 5.5122 mL
15 mM 0.1470 mL 0.7350 mL 1.4699 mL 3.6748 mL
20 mM 0.1102 mL 0.5512 mL 1.1024 mL 2.7561 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱(chēng)：
SB-590885
目錄號(hào)：
HY-10966
需求量：