Gefitinib (吉非替尼)

Gefitinib (ZD1839) 是一種有效，選擇性和口服活性的 EGFR 酪氨酸激酶抑制劑，IC50 為 33 nM。Gefitinib 選擇性抑制 EGF 刺激的腫瘤細胞生長 (IC50 為 54 nM)，并阻斷 EGF 刺激的腫瘤細胞中 EGFR 自磷酸化。Gefitinib 還可誘導(dǎo)細胞自噬 (autophagy) 和凋亡 (apoptosis)，可用于ai相關(guān)的研究

貨號：HY-50895
CAS：

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-50895

起訂量：1

規(guī)格:：100mg

價格:：￥550

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產(chǎn)品詳情

Gefitinib (Synonyms: 吉非替尼）

生物活性

Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer ^[1]^[2]^[5].

IC₅₀ & Target：EGFR

體外研究(In Vitro)

Gefitinib (0.01–0.1? μM, 72 h) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth^[2].
Gefitinib (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth^[2].
Gefitinib (0.62 μM, 24-72 h) inhibits IL-13-induced M2-like polarization of RAW 264.7 cells through the STAT6-dependent signaling pathway^[3].
Gefitinib (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration^[3].
Gefitinib (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells)^[4].

Cell Line:	NR6wtEGFR, NR6W and NR6M
Concentration:	1, 10, 100 μM
Incubation Time:	5?h
Result:	Inhibited EGFR tyrosine phosphorylations.

體內(nèi)研究(In Vivo)

Gefitinib (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model^[3].
Gefitinib (Oral administration, 75 mg/kg for the initial week, daily for 5 consecutive days per week) eliminates phosphorylation of HER2 and HER3 and signaling through MAPK and Akt in lobular hyperplasias and carcinomas, increases MAPK activity and cytokine production in splenocytes and lymph nodes^[5].

Animal Model:	LLC mice metastasis model^[3]
Dosage:	75 mg/kg/d, for 21 days.
Administration:	Oral administration
Result:	Reduced the number of lung metastasis nodules, down-regulated the expression of M2 marker genes and the percentages CD206⁺ and CD68⁺ macrophages in tumor tissues.

分子量：446.90

Formula：C₂₂H₂₄ClFN₄O₃

CAS 號：184475-35-2

中文名稱：吉非替尼；吉菲替尼

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	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

In Vitro:

DMSO : 250 mg/mL (559.41 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.2376 mL	11.1882 mL	22.3764 mL
5 mM	0.4475 mL	2.2376 mL	4.4753 mL
10 mM	0.2238 mL	1.1188 mL	2.2376 mL

*

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, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

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

1.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution
4.

請依序添加每種溶劑： 1% DMSO 99% saline
Solubility: 0.5 mg/mL (1.12 mM); Suspended solution; Need ultrasonic

參考文獻

[1]. Wakeling AE, et al. ZD1839: an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62(20):5749-54.

[2]. Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23.

[3]. Muhammad Tariq, et al. Gefitinib inhibits M2-like polarization of tumor-associated macrophages in Lewis lung cancer by targeting the STAT6 signaling pathway. Acta Pharmacol Sin. 2017 Nov;38(11):1501-1511.

[4]. Mark S Cragg, et al. Gefitinib-induced killing of NSCLC cell lines expressing mutant EGFR requires BIM and can be enhanced by BH3 mimetics. PLoS Med. 2007 Oct;4(10):1681-89; discussion 1690.

[5]. Marie P Piechocki, et al. Gefitinib prevents cancer progression in mice expressing the activated rat HER2/neu. Int J Cancer. 2008 Apr 15;122(8):1722-9.

Gefitinib (吉非替尼)

Gefitinib (ZD1839) 是一種有效，選擇性和口服活性的 EGFR 酪氨酸激酶抑制劑，IC50 為 33 nM。Gefitinib 選擇性抑制 EGF 刺激的腫瘤細胞生長 (IC50 為 54 nM)，并阻斷 EGF 刺激的腫瘤細胞中 EGFR 自磷酸化。Gefitinib 還可誘導(dǎo)細胞自噬 (autophagy) 和凋亡 (apoptosis)，可用于ai相關(guān)的研究

貨號：HY-50895
CAS：

品牌：MCE

型號：HY-50895

起訂量：1

規(guī)格:：100mg

價格:：￥550

15906629305

在線客服

客服一

產(chǎn)品詳情

Gefitinib (Synonyms: 吉非替尼）

生物活性

Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer ^[1]^[2]^[5].

IC₅₀ & Target：EGFR

體外研究(In Vitro)

Gefitinib (0.01–0.1? μM, 72 h) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth^[2].
Gefitinib (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth^[2].
Gefitinib (0.62 μM, 24-72 h) inhibits IL-13-induced M2-like polarization of RAW 264.7 cells through the STAT6-dependent signaling pathway^[3].
Gefitinib (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration^[3].
Gefitinib (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells)^[4].

Cell Line:	NR6wtEGFR, NR6W and NR6M
Concentration:	1, 10, 100 μM
Incubation Time:	5?h
Result:	Inhibited EGFR tyrosine phosphorylations.

體內(nèi)研究(In Vivo)

Gefitinib (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model^[3].
Gefitinib (Oral administration, 75 mg/kg for the initial week, daily for 5 consecutive days per week) eliminates phosphorylation of HER2 and HER3 and signaling through MAPK and Akt in lobular hyperplasias and carcinomas, increases MAPK activity and cytokine production in splenocytes and lymph nodes^[5].

Animal Model:	LLC mice metastasis model^[3]
Dosage:	75 mg/kg/d, for 21 days.
Administration:	Oral administration
Result:	Reduced the number of lung metastasis nodules, down-regulated the expression of M2 marker genes and the percentages CD206⁺ and CD68⁺ macrophages in tumor tissues.

分子量：446.90

Formula：C₂₂H₂₄ClFN₄O₃

CAS 號：184475-35-2

中文名稱：吉非替尼；吉菲替尼

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	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

In Vitro:

DMSO : 250 mg/mL (559.41 mM; Need ultrasonic)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.2376 mL	11.1882 mL	22.3764 mL
5 mM	0.4475 mL	2.2376 mL	4.4753 mL
10 mM	0.2238 mL	1.1188 mL	2.2376 mL

*

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, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

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

1.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution
4.

請依序添加每種溶劑： 1% DMSO 99% saline
Solubility: 0.5 mg/mL (1.12 mM); Suspended solution; Need ultrasonic

參考文獻

[1]. Wakeling AE, et al. ZD1839: an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62(20):5749-54.

[2]. Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23.

[3]. Muhammad Tariq, et al. Gefitinib inhibits M2-like polarization of tumor-associated macrophages in Lewis lung cancer by targeting the STAT6 signaling pathway. Acta Pharmacol Sin. 2017 Nov;38(11):1501-1511.

[4]. Mark S Cragg, et al. Gefitinib-induced killing of NSCLC cell lines expressing mutant EGFR requires BIM and can be enhanced by BH3 mimetics. PLoS Med. 2007 Oct;4(10):1681-89; discussion 1690.

[5]. Marie P Piechocki, et al. Gefitinib prevents cancer progression in mice expressing the activated rat HER2/neu. Int J Cancer. 2008 Apr 15;122(8):1722-9.

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Gefitinib (Synonyms: 吉非替尼）

Gefitinib (吉非替尼)

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Gefitinib (Synonyms: 吉非替尼）