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  2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. AZ-5104

AZ-5104 是 AZD 9291 的活性，去甲基化代謝物。AZ-5104 是 EGFR 抑制劑；抑制 EGFRL858R/T790M，EGFRL858R，EGFRL861Q，EGFR 和 ErbB4 的 IC50 值分別為1，6，1，25 和 7 nM。

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AZ-5104 Chemical Structure

AZ-5104 Chemical Structure

CAS No. : 1421373-98-9

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥610
In-stock
5 mg ￥500
In-stock
10 mg ￥800
In-stock
50 mg ￥2400
In-stock
100 mg ￥3600
In-stock
200 mg ￥4050
In-stock
500 mg   詢價  
1 g   詢價  

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Customer Review

Other Forms of AZ-5104:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively.

IC50 & Target[1]

EGFRL858R/T790M

1 nM (IC50)

EGFRL858R

1 nM (IC50)

EGFRL861Q

6 nM (IC50)

EGFR

25 nM (IC50)

ErbB4

7 nM (IC50)

EGFRExon 19 deletion/T790M

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
Calu-3 GI50
58 nM
Compound: 27
Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
[PMID: 25271963]
LoVo IC50
33 nM
Compound: AZ5104
Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
[PMID: 26968253]
LoVo IC50
33 μM
Compound: 27
Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
[PMID: 25271963]
NCI-H1975 GI50
16 nM
Compound: 27
Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
[PMID: 25271963]
NCI-H1975 IC50
2 μM
Compound: 27
Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
[PMID: 25271963]
PC-9 IC50
2 nM
Compound: AZ5104
Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
[PMID: 26968253]
PC-9 IC50
2 μM
Compound: 27
Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
[PMID: 25271963]
PC-9 GI50
21 nM
Compound: 27
Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
[PMID: 25271963]
體外研究
(In Vitro)

AZ-5104 inhibits EGFR phosphorylation with IC50s of 2, 1, 2, 53, and 33 nM in H1975 (EGFRL858R/T790M), PC-9VanR (EGFRExon 19 deletion/T790M), PC-9 (EGFRExon 19 deletion), H2073 (WT), and LOVO (WT), respectively. AZ5104 exhibits a reduced selectivity margin against wild-type EGFR when compared to AZD9291. AZ5104 display minimal off-target activity against other non-HER family kinases, but has the potential to target both HER2 and HER4 kinase activity[1].

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

The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice[1].

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

485.58

Formula

C27H31N7O2
CAS 號
性狀

固體

顏色

White to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
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)胞實驗： 

DMSO 中的溶解度 : ≥ 28 mg/mL (57.66 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.0594 mL 10.2970 mL 20.5939 mL
5 mM 0.4119 mL 2.0594 mL 4.1188 mL
查看完整儲備液配制表

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

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，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

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.15 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

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

    Solubility: 2.5 mg/mL (5.15 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 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。
動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動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， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲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: 99.69%

參考文獻(xiàn)
Cell Assay
[1]

Cells were treated for 2 h with a dose-response of each drug (AZ-5104). Wild-type cells were stimulated for 10 minutes with 25 ng/mL of EGF before lysis. Level of EGFR phosphorylation was quantified in cell extracts using ELISA[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1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 2.0594 mL 10.2970 mL 20.5939 mL 51.4848 mL
5 mM 0.4119 mL 2.0594 mL 4.1188 mL 10.2970 mL
10 mM 0.2059 mL 1.0297 mL 2.0594 mL 5.1485 mL
15 mM 0.1373 mL 0.6865 mL 1.3729 mL 3.4323 mL
20 mM 0.1030 mL 0.5148 mL 1.0297 mL 2.5742 mL
25 mM 0.0824 mL 0.4119 mL 0.8238 mL 2.0594 mL
30 mM 0.0686 mL 0.3432 mL 0.6865 mL 1.7162 mL
40 mM 0.0515 mL 0.2574 mL 0.5148 mL 1.2871 mL
50 mM 0.0412 mL 0.2059 mL 0.4119 mL 1.0297 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：
AZ-5104
目錄號：
HY-B0793
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