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  2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  3. EGFR Autophagy Apoptosis
  4. PD168393

PD168393 是有效、選擇性和細胞滲透性的 EGFR 酪氨酸激酶 (EGFR tyrosine kinase) 和 ErbB2 的抑制劑。PD168393 不可逆轉(zhuǎn)地失活 EGF 受體 (IC50=0.7 nM)，但對胰島素受體、PDGFR、FGFR 和 PKC 無作用。

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PD168393 Chemical Structure

PD168393 Chemical Structure

CAS No. : 194423-15-9

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥625
In-stock
2 mg ￥550
In-stock
5 mg ￥770
In-stock
10 mg ￥1300
In-stock
25 mg ￥2600
In-stock
50 mg ￥4600
In-stock
100 mg   詢價  
200 mg   詢價  

* Please select Quantity before adding items.

Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

PD168393?is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC[1].

IC50 & Target[1]

EGFR

0.7 nM (IC50)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
0.012 μM
Compound: 2, PD-168393
Inhibition of EGFR autophosphorylation in human A431 cells after 1 hr by Western blot
Inhibition of EGFR autophosphorylation in human A431 cells after 1 hr by Western blot
[PMID: 20151670]
A-431 IC50
0.036 μM
Compound: PD168393
Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide substrate by ELISA
Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide substrate by ELISA
[PMID: 27135370]
A-431 IC50
0.152 μM
Compound: 2, PD-168393
Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by Western blot
Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by Western blot
[PMID: 20151670]
A-431 IC50
1.96 μM
Compound: PD168393
Antiproliferative activity against human A431 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human A431 cells assessed as cell growth inhibition after 72 hrs by MTT assay
[PMID: 27135370]
A-431 IC50
1.96 μM
Compound: 3, PD-168393
Antiproliferative activity against human A431 cells after 72 hrs by MTT assay
Antiproliferative activity against human A431 cells after 72 hrs by MTT assay
[PMID: 17154492]
A-431 IC50
2.7 nM
Compound: 3
Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting
Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting
[PMID: 10753475]
A549 IC50
17.9 nM
Compound: 2, PD168393
Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by Western blot analysis
Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by Western blot analysis
[PMID: 23988354]
A549 IC50
3.94 nM
Compound: 2, PD168393
Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by Western blot analysis
Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by Western blot analysis
[PMID: 23988354]
BaF3 GI50
< 0.5 μM
Compound: 3b
Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay
Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 mutant after 96 hrs by cell titer-glo assay
[PMID: 20222733]
BaF3 GI50
< 0.5 μM
Compound: 3b
Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay
Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 mutant after 96 hrs by cell titer-glo assay
[PMID: 20222733]
BaF3 GI50
< 0.5 μM
Compound: 3b
Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay
Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 mutant after 96 hrs by cell titer-glo assay
[PMID: 20222733]
BaF3 GI50
< 0.5 μM
Compound: 3b
Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay
Growth inhibition of mouse BA/F3 cells expressing EGFR L858R mutant after 96 hrs by cell titer-glo assay
[PMID: 20222733]
BaF3 GI50
< 0.5 μM
Compound: 3b
Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 and Thr790Met mutant after 96 hrs by cell titer-glo assay
Growth inhibition of mouse BA/F3 cells expressing EGFR Del3 and Thr790Met mutant after 96 hrs by cell titer-glo assay
[PMID: 20222733]
BaF3 GI50
< 0.5 μM
Compound: 3b
Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 and Thr790Met mutant after 96 hrs by cell titer-glo assay
Growth inhibition of mouse BA/F3 cells expressing EGFR Del5 and Thr790Met mutant after 96 hrs by cell titer-glo assay
[PMID: 20222733]
BaF3 GI50
< 0.5 μM
Compound: 3b
Growth inhibition of mouse BA/F3 cells expressing EGFR L858R and Thr790Met mutant after 96 hrs by cell titer-glo assay
Growth inhibition of mouse BA/F3 cells expressing EGFR L858R and Thr790Met mutant after 96 hrs by cell titer-glo assay
[PMID: 20222733]
BaF3 GI50
> 0.5 μM
Compound: 3b
Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 and Thr790Met mutant after 96 hrs by cell titer-glo assay
Growth inhibition of mouse BA/F3 cells expressing EGFR Del1 and Thr790Met mutant after 96 hrs by cell titer-glo assay
[PMID: 20222733]
NCI-H1975 IC50
0.028 μM
Compound: I
Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as inhibition of EGF-mediated autophosphorylation incubated for 30 mins prior to EGF challenge by cytoblot assay
Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as inhibition of EGF-mediated autophosphorylation incubated for 30 mins prior to EGF challenge by cytoblot assay
10.1039/C3MD00118K
NCI-H1975 IC50
0.44 μM
Compound: I
Cytotoxicity against gefitinib-resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay
Cytotoxicity against gefitinib-resistant human NCI-H1975 cells expressing EGFR L858R/T790M double mutant assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay
10.1039/C3MD00118K
NCI-H1975 IC50
0.61 μM
Compound: 2, PD-168393
Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
[PMID: 20151670]
Sf9 IC50
< 0.001 μM
Compound: 2, PD-168393
Inhibition of human recombinant EGFR expressed in baculovirus-infected Sf9 cells by radioactive phosphotransfer assay
Inhibition of human recombinant EGFR expressed in baculovirus-infected Sf9 cells by radioactive phosphotransfer assay
[PMID: 17334377]
SK-BR-3 IC50
0.015 μM
Compound: 2
Inhibition of cell growth of SKBr3 cell lines using cell-based assay
Inhibition of cell growth of SKBr3 cell lines using cell-based assay
[PMID: 11495584]
SK-BR-3 IC50
0.2 μM
Compound: I
Cytotoxicity against human SKBR3 cells expressing wild type EGFR assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay
Cytotoxicity against human SKBR3 cells expressing wild type EGFR assessed as growth inhibition incubated for 1 hr prior to EGF challenge measured after 72 hrs by luciferase reporter gene assay
10.1039/C3MD00118K
SW-620 IC50
4.133 μM
Compound: 2
Inhibition of cell growth of SW620 cell lines using cell-based assay
Inhibition of cell growth of SW620 cell lines using cell-based assay
[PMID: 11495584]
SW-620 IC50
8.23 μM
Compound: 2, PD-168393
Cytotoxicity against human SW620 cells after 72 hrs by MTT assay
Cytotoxicity against human SW620 cells after 72 hrs by MTT assay
[PMID: 20151670]
體外研究
(In Vitro)

PD168393 inhibits ligand-dependent receptor phosphorylation and?inhibits EGF-induced tyrosine phosphorylation in A431 cells and Heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 values of 4.3? nM and 5.7? nM, respectively[1].

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

PD168393 (intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28) is effective?in vivo, and produces tumor growth inhibition of 115% after 15 days’ treatment in human epidermoid carcinoma xenografts in mice[1].

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

Animal Model: A431 human epidermoid carcinoma grown as a xenograft in nude mice[1]
Dosage: 58 mg/kg
Administration: Intraperitoneal injection; 58 mg/kg; once daily; days 10-14, 17-21, and 24-28
Result: Suppressed the growth of human epidermoid carcinoma xenografts.
分子量

369.22

Formula

C17H13BrN4O
CAS 號
性狀

固體

顏色

Light yellow to khaki

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)
細胞實驗： 

DMSO 中的溶解度 : ≥ 30 mg/mL (81.25 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 2.7084 mL 13.5421 mL 27.0841 mL
5 mM 0.5417 mL 2.7084 mL 5.4168 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?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，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
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 (6.77 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。

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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： 50% PEG300    50% Saline

    Solubility: 3.33 mg/mL (9.02 mM); 懸濁液; 超聲助溶

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
參考文獻

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 2.7084 mL 13.5421 mL 27.0841 mL 67.7103 mL
5 mM 0.5417 mL 2.7084 mL 5.4168 mL 13.5421 mL
10 mM 0.2708 mL 1.3542 mL 2.7084 mL 6.7710 mL
15 mM 0.1806 mL 0.9028 mL 1.8056 mL 4.5140 mL
20 mM 0.1354 mL 0.6771 mL 1.3542 mL 3.3855 mL
25 mM 0.1083 mL 0.5417 mL 1.0834 mL 2.7084 mL
30 mM 0.0903 mL 0.4514 mL 0.9028 mL 2.2570 mL
40 mM 0.0677 mL 0.3386 mL 0.6771 mL 1.6928 mL
50 mM 0.0542 mL 0.2708 mL 0.5417 mL 1.3542 mL
60 mM 0.0451 mL 0.2257 mL 0.4514 mL 1.1285 mL
80 mM 0.0339 mL 0.1693 mL 0.3386 mL 0.8464 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：
PD168393
目錄號：
HY-13896
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