Tyrphostin 25 (AG82) is a specific inhibitor of the EGFR tyrosine kinase. Tyrphostin 25 is also a GPR35 agonist with an IC₅₀ of 0.94 µM and an EC₅₀ of 5.3 µM^[1][2].

EGFR tyrosine kinase^[1]
IC₅₀: 0.94 µM (GPR35)^[2]
EC₅₀: 5.3 µM (GPR35)^[2]

202.17

C₁₀H₆N₂O₃

118409-58-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Klemke RL, et al. Receptor tyrosine kinase signaling required for integrin alpha v beta 5-directed cell motility but not adhesion on vitronectin. J Cell Biol. 1994 Nov;127(3):859-66.

  [2]. Deng H, et al. Tyrphostin analogs are GPR35 agonists. FEBS Lett. 2011 Jun 23;585(12):1957-62.

(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor^[1].

(E)-AG 99 effectively blocks tyrosine phosphorylation of p145^met and promotes cell death accompanied by activation of caspase-like proteases^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

204.18

C₁₀H₈N₂O₃

122520-85-8

Room temperature in continental US; may vary elsewhere.

DMSO : 165 mg/mL (808.11 mM; Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.75 mg/mL (13.47 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (13.47 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.75 mg/mL (13.47 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (13.47 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

• [1]. Yamamoto N, et al. Tyrosine phosphorylation of p145met mediated by EGFR and Src is required for serum-independent survival of human bladder carcinoma cells. J Cell Sci. 2006 Nov 15;119(Pt 22):4623-33.

AG 555 (Tyrphostin AG 555), a potent antiretroviral drug, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation^[1][2].

AG 555 (100 μM) inhibits both the early stages (integration process) and the late stages (viral protein synthesis) in the virus life cycle^[1].
Tyrphostins AG555, which blocks Cdk2 activation, induces growth arrest of immortalized cells at G1-S and early S and is very effective in arresting the growth of EGFR overexpressor cells^[2].
Tyrphostin AG 555 can selectively suppress BPV-1 transcription through MAP kinase pathway activation and binding of phosphorylated Jun/ATF-2 at a novel intragenic regulatory sequence^[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

322.36

C₁₉H₁₈N₂O₃

133550-34-2

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL (310.21 mM)

* “≥” means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (7.76 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.76 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (7.76 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.76 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

• [1]. Seri E Aflalo, et al. Tyrphostin AG-555 inhibits early and late stages of Moloney murine leukemia virus replication cycle. International Journal of Oncology. 1997.

  [2]. Nir Osherov, et al. Tyrphostin AG494 blocks Cdk2 activation Nir Osherov. FEBS Letters 410 (1997) 187-190.

  [3]. Sabine Baars, et al. Tyrphostin AG 555 Inhibits Bovine Papillomavirus Transcription by Changing the Ratio between E2 Transactivator/Repressor Function. Vol. 278, No. 39, Issue of September 26, pp. 37306–37313, 2003.

AG-1478 (Tyrphostin AG-1478) is a selective EGFR tyrosine kinase inhibitor with IC₅₀ of 3 nM. AG-1478 has antiviral effects against HCV and encephalomyocarditis virus (EMCV).

AG-1478 (AG1478) is irreversible for growth regulation of human lung (A549) and prostate (DU145) cancer cell lines, cultured in chemically defined DMEM/F12 medium. AG-1478 seems to be more effective at lower concentrations, but is unable to completely inhibit growth of A549 cells^[1]. Inhibition of EGFR by specific tyrosine kinase inhibitor AG-1478 (AG1478) significantly decreases the angiotensin II-mediated synthesis of TGF-β and fibronectin by cardiac fibroblasts. EGFR is pharmacologically inhibited by small-molecule inhibitor AG-1478 with IC₅₀ of 4 nM^[2]. Both Polyfect (PF) and Superfect (SF) treatment lead to increased apoptosis in HEK 293 cells to a similar extent as assessed by flow cytometry. The antioxidant, tempol, significantly reduced dendrimer-mediated apoptosis for both PF and SF. AG-1478 (AG1478), at a 10-fold higher dose (100 μM) than used in signaling studies, is used as a positive control and significantly induced apoptosis in HEK 293 cells^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Administration of AG-1478 (AG1478) significantly reduces myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. ApoE^-/- mice are first fed with HFD for 8 weeks (ApoE-HFD), and then administrated with AG-1478 (10 mg/kg/day) or 542 (10 mg/kg/day) for another 8 weeks by oral gavage. AG-1478 or 542 treatment blocks HFD induced cardiac EGFR phosphorylation in vivo, without affecting the plasma level of low density lipoprotein (LDL) and total triglyceride (TG)^[2]. Administration of EGF (10 nM) leads to a robust and reproducible elevation in EGFR phosphorylation that can be blocked by AG-1478 (AG1478), a known inhibitor of EGFR phosphorylation. Increasing doses of Polyfect (PF) result in a significant reduction in EGF-induced EGFR phosphorylation (p<0.05) but this is to a lesser extent than observed with AG1478^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

315.75

C₁₆H₁₄ClN₃O₂

153436-53-4

酪氨酸磷酸化抑制剂 AG-1478

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL (316.71 mM)

* “≥” means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 1% CMC  0.5% Tween-80

  Solubility: 5 mg/mL (15.84 mM); Suspended solution; Need ultrasonic
• 2.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 3.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 4.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.59 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Bojko A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol. 2012 Jul 5;50(2):186-95.

  [2]. Li W, et al. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580.

  [3]. Akhtar S, et al. Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling In Vitro and In Vivo. PLoS One. 2015 Jul 13;10(7):e0132215.

  [4]. Dorobantu CM, et al. Tyrphostin AG1478 Inhibits Encephalomyocarditis Virus and Hepatitis C Virus by Targeting Phosphatidylinositol 4-Kinase IIIα. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6402-6.

DU145 (HTB-81) and A549 (CCL-185) cells are seeded on 96-well plates at concentrations of 4×10³ cells/well in MEM (DU145 cells) or DMEM (A549 cells). Following 24 h of incubation, the culture medium is replaced with serum-free DMEM/F12 (1:1) supplemented with Transferrin (5 mg/mL), sodium selenite (2 ng/mL) and albumin (0.5 mg/mL) [DMEM/F12+]. After an additional 24 h of incubation (Day 0), the medium is replaced by serum-free DMEM/F12+ medium containing tyrosine kinase inhibitors: AG494, AG-1478 respectively in concentration ranges 1-20 μM and 0.1-8 μM. The incubation is continued for the next 24 h at 37°C in a humidified atmosphere. The modified crystal violet staining method (CV) and MTT assay are used to determine the influence of the tyrphostins on the proliferation of target cells. The absorbance is measured using a Tecan multiscan plate recorder^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[2]
28 C57BL/6 or ApoE^-/- mice are randomly divided into four weight-matched groups. 7 mice are fed with standard animal low-fat diet containing 10 kcal.% fat, 20 kcal.% protein and 70 kcal.% carbohydrate serve as a normal control group (Control or ApoE-LF), while the remaining 21 mice are fed with high-fat diet containing 60 kcal.% fat, 20 kcal.% protein and 20 kcal.% carbohydrate for 16 weeks. Since 9^th week, AG-1478 or 542 are given daily by oral gavage at a dose of 10 mg/kg/day for the next 8 weeks. Mice in the Control and HFD groups are gavaged with vehicle (1% CMC-Na solution) only. At the day before the sacrifice of ApoE^-/- mice, doppler analysis is performed to determine the pathologic cardiac hypertrophy.
Rats^[3]
Male Wistar rats weighing about 300g are used in this study and divided into the following groups (N=5). Group 1: Non-diabetic (Control, C) animals, Group 2: C+PF (10mg/kg administered as a single intraperotoneal (i.p) injection) Group 3: C+SF (10mg/kg i.p); Group 4: C+AG-1478 (1 mg/kg i.p). Group 5: Rats bearing 4 weeks of diabetes (D) induced by a single i.p. injection of streptozotocin (55 mg/kg body weight); Group 6: D+PF (10 mg/kg i.p) Group 7: D+SF (10 mg/kg i.p) and Group 8: D+AG-1478 (1 mg/kg i.p). AG-1478 and dendrimer treatments are administered as single dose for 24h prior to sacrifice. Rat body weight and basal glucose levels are assessed before and after treatments just before sacrificing the animals. An automated blood glucose analyzer is used to assess blood glucose concentrations and rats with a blood glucose concentration above 250 mg/dL (approx. 14 mM) are declared diabetic as in previous studies.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Bojko A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol. 2012 Jul 5;50(2):186-95.

  [2]. Li W, et al. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice. Sci Rep. 2016 Apr 18;6:24580.

  [3]. Akhtar S, et al. Cationic Polyamidoamine Dendrimers as Modulators of EGFR Signaling In Vitro and In Vivo. PLoS One. 2015 Jul 13;10(7):e0132215.

  [4]. Dorobantu CM, et al. Tyrphostin AG1478 Inhibits Encephalomyocarditis Virus and Hepatitis C Virus by Targeting Phosphatidylinositol 4-Kinase IIIα. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6402-6.

AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC₅₀ of 7 μM. AG1024 inhibits phosphorylation of IR (IC₅₀=57 μM). AG1024 induces apoptosis and has anti-cancer activity^[1][2].

IC50: 7 μM (IGF1R) and 57 μM (IR)^[1][2]

AG1024 (Tyrphostin AG 1024; 2-10 μM; 1-5 days) shows a dose-dependent inhibition of cell proliferation^[1].
AG1024 (1-5 μM; 1-3 days) induces UT7-9 and Baf3-p210 cells apoptosis^[1].
AG1024 (2 μM; 6, 12 hours) downregulates phospho-Akt, Bcr-Abl and upregulates DNA-PKcs^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

AG1024 (Tyrphostin AG 1024; 30 μg; i.p.; per day; for 2 weeks) significantly delays the tumour growth^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

305.17

C₁₄H₁₃BrN₂O

65678-07-1

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 50 mg/mL (163.84 mM)

* “≥” means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• [1]. Párrizas M, et al. Specific inhibition of IGF-1R and IR tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33.

  [2]. Deutsch E, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. Br J Cancer. 2004 Nov 1;91(9):1735-41.