TIE-2/VEGFR-2 kinase-IN-2

发表于2025年1月10日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TIE-2/VEGFR-2 kinase-IN-2

TIE-2/VEGFR-2 kinase-IN-2 是一种有效的 VEGFR2 和 Tie-2 双抑制剂，pIC₅₀ 值分别为 8.61 和 8.56。TIE-2/VEGFR-2 kinase-IN-2 是一种抗血管生成剂，可用于癌症研究。

TIE-2/VEGFR-2 kinase-IN-2 Chemical Structure

CAS No. : 501693-48-7

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生物活性

TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC₅₀ values of 8.61 and 8.56, respectively^[1]. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research^[2].

IC₅₀ & Target^[1]

VEGFR-2

Tie-2

分子量

431.34

Formula

C₂₀H₁₃F₄N₅O₂

CAS 号

501693-48-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Yasushi Miyazaki, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8.

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TIE-2/VEGFR-2 kinase-IN-2

发表于2025年1月10日由上海金畔生物科技有限公司

TIE-2/VEGFR-2 kinase-IN-2

TIE-2/VEGFR-2 kinase-IN-2 Chemical Structure

CAS No. : 501693-48-7

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生物活性

IC₅₀ & Target^[1]

VEGFR-2

Tie-2

分子量

431.34

Formula

C₂₀H₁₃F₄N₅O₂

CAS 号

501693-48-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Yasushi Miyazaki, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8.

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TIE-2/VEGFR-2 kinase-IN-2

发表于2025年1月10日由上海金畔生物科技有限公司

TIE-2/VEGFR-2 kinase-IN-2

TIE-2/VEGFR-2 kinase-IN-2 Chemical Structure

CAS No. : 501693-48-7

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生物活性

IC₅₀ & Target^[1]

VEGFR-2

Tie-2

分子量

431.34

Formula

C₂₀H₁₃F₄N₅O₂

CAS 号

501693-48-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Yasushi Miyazaki, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8.

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VEGFR-2-IN-20

发表于2024年12月31日由上海金畔生物科技有限公司

VEGFR-2-IN-20

VEGFR-2-IN-20 (Compound 7) 是一种有效的 VEGFR 抑制剂。 VEGFR-2-IN-20 具有研究癌症疾病的潜力。

VEGFR-2-IN-20 Chemical Structure

CAS No. : 2404581-25-3

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生物活性	VEGFR-2-IN-20 (Compound 7) is a potent inhibitor of VEGFR. VEGFR-2-IN-20 has the potential for the research of cancer diseases^[1].
分子量	396.46
Formula	C₂₀H₂₀N₄O₃S
CAS 号	2404581-25-3
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Eissa IH, et al. Discovery of new quinazolin-4(3H)-ones as VEGFR-2 inhibitors: Design, synthesis, and anti-proliferative evaluation. Bioorg Chem. 2020;105:104380.

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VEGFR-2-IN-10

发表于2024年12月24日由上海金畔生物科技有限公司

VEGFR-2-IN-10

VEGFR-2-IN-10 在没有细胞毒性作用的情况下，对 VEGF 诱导的 VEGFR2 磷酸化具有增强的抗血管生成效力（IC₅₀ = 0.7 μM）。

VEGFR-2-IN-10 Chemical Structure

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生物活性	VEGFR-2-IN-10 exhibits increased antiangiogenic potency (IC₅₀ = 0.7 μM) against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects.
分子量	335.40
Formula	C₂₀H₂₁N₃O₂
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Cho SM, et al. Development of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact. J Med Chem. 2021 Nov 11;64(21):15858-15867.

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VEGFR-2-IN-10

发表于2024年12月24日由上海金畔生物科技有限公司

VEGFR-2-IN-10

VEGFR-2-IN-10 在没有细胞毒性作用的情况下，对 VEGF 诱导的 VEGFR2 磷酸化具有增强的抗血管生成效力（IC₅₀ = 0.7 μM）。

VEGFR-2-IN-10 Chemical Structure

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生物活性	VEGFR-2-IN-10 exhibits increased antiangiogenic potency (IC₅₀ = 0.7 μM) against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects.
分子量	335.40
Formula	C₂₀H₂₁N₃O₂
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Cho SM, et al. Development of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact. J Med Chem. 2021 Nov 11;64(21):15858-15867.

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VEGFR-2-IN-10

发表于2024年12月24日由上海金畔生物科技有限公司

VEGFR-2-IN-10

VEGFR-2-IN-10 在没有细胞毒性作用的情况下，对 VEGF 诱导的 VEGFR2 磷酸化具有增强的抗血管生成效力（IC₅₀ = 0.7 μM）。

VEGFR-2-IN-10 Chemical Structure

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生物活性	VEGFR-2-IN-10 exhibits increased antiangiogenic potency (IC₅₀ = 0.7 μM) against VEGF-induced VEGFR2 phosphorylation without cytotoxic effects.
分子量	335.40
Formula	C₂₀H₂₁N₃O₂
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Cho SM, et al. Development of Novel VEGFR2 Inhibitors Originating from Natural Product Analogues with Antiangiogenic Impact. J Med Chem. 2021 Nov 11;64(21):15858-15867.

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VEGFR-IN-1

发表于2024年12月6日由上海金畔生物科技有限公司

VEGFR-IN-1

VEGFR-IN-1 (compound 3) 是一种有效的血管生成抑制剂，对于 KDR、Flt-1、c-Kit、EGF-R 和 c-Src，IC₅₀ 分别为 0.02、0.18、0.24、7.3 和 7 µM。

VEGFR-IN-1 Chemical Structure

CAS No. : 269390-69-4

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生物活性

VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC₅₀s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively^[1].

IC₅₀ & Target^[1]

KDR

0.02 μM (IC₅₀)

Flt-1

0.18 μM (IC₅₀)

EGFR

0.24 μM (IC₅₀)

分子量

337.80

Formula

C₁₉H₁₆ClN₃O

CAS 号

269390-69-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Furet P, et al. Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg Med Chem Lett. 2003;13(18):2967-2971.

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VEGFR-IN-1

发表于2024年12月6日由上海金畔生物科技有限公司

VEGFR-IN-1

VEGFR-IN-1 (compound 3) 是一种有效的血管生成抑制剂，对于 KDR、Flt-1、c-Kit、EGF-R 和 c-Src，IC₅₀ 分别为 0.02、0.18、0.24、7.3 和 7 µM。

VEGFR-IN-1 Chemical Structure

CAS No. : 269390-69-4

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生物活性

VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC₅₀s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively^[1].

IC₅₀ & Target^[1]

KDR

0.02 μM (IC₅₀)

Flt-1

0.18 μM (IC₅₀)

EGFR

0.24 μM (IC₅₀)

分子量

337.80

Formula

C₁₉H₁₆ClN₃O

CAS 号

269390-69-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Furet P, et al. Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg Med Chem Lett. 2003;13(18):2967-2971.

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VEGFR-IN-1

发表于2024年12月6日由上海金畔生物科技有限公司

VEGFR-IN-1

VEGFR-IN-1 (compound 3) 是一种有效的血管生成抑制剂，对于 KDR、Flt-1、c-Kit、EGF-R 和 c-Src，IC₅₀ 分别为 0.02、0.18、0.24、7.3 和 7 µM。

VEGFR-IN-1 Chemical Structure

CAS No. : 269390-69-4

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生物活性

VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC₅₀s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively^[1].

IC₅₀ & Target^[1]

KDR

0.02 μM (IC₅₀)

Flt-1

0.18 μM (IC₅₀)

EGFR

0.24 μM (IC₅₀)

分子量

337.80

Formula

C₁₉H₁₆ClN₃O

CAS 号

269390-69-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Furet P, et al. Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg Med Chem Lett. 2003;13(18):2967-2971.

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VEGFR-2-IN-19

发表于2024年12月3日由上海金畔生物科技有限公司

VEGFR-2-IN-19

VEGFR-2-IN-19 (Compound 15b) 是一种有效的 VEGFR2 抑制剂。VEGFR-2-IN-19 诱导细胞凋亡 (apoptosis)，增加细胞内活性氧 (reactive oxygen species) 水平。VEGFR-2-IN-19 可以用作抗癌剂。

VEGFR-2-IN-19 Chemical Structure

CAS No. : 2456315-41-4

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生物活性

VEGFR-2-IN-19 (Compound 15b) is a potent VEGFR2 inhibitor. VEGFR-2-IN-19 induces cell apoptosis and increases intracellular reactive oxygen species level. VEGFR-2-IN-19 can be used as an anticancer agent^[1].

IC₅₀ & Target

VEGFR2

体外研究
(In Vitro)

VEGFR-2-IN-19 (Compound 15b) (0-100 µM, 48 h) shows antiproliferative activity against cancer cells^[1].
VEGFR-2-IN-19 (0-10 µM, 48 h) inhibits the phosphorylation of VEGFR2 and the Raf/MEK/ERK signaling pathway, induces cell apoptosis, and arrests cell cycle at G0/G1 phase in HT-29 cells^[1].
VEGFR-2-IN-19 (0-10 µM, 12 h) increases intracellular reactive oxygen species level in HT-29 cells^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:	HT-29 and A549
Concentration:	0-100 µM
Incubation Time:	48 h
Result:	Showed antiproliferative activity with IC₅₀ values of 3.38±1.3 µM and 0.63±0.04 µM against HT-29 and A549 cells, respectively.

Western Blot Analysis^[1]

Cell Line:	HT-29
Concentration:	0, 1, 5, and 10 µM
Incubation Time:	48 h
Result:	Effectively inhibited the phosphorylation of VEGFR2 in dose-dependent manner. Suppressed dose-dependently expression of c-Raf, ERK1/2, and MEK and phosphorylation of ERK1/2 (pERK1/2). Up-regulated caspase-3 and Bax expression, down-regulated Bcl-2 expression.

Apoptosis Analysis^[1]

Cell Line:	HT-29
Concentration:	0, 1, 5, and 10 µM
Incubation Time:	48 h
Result:	The total numbers of early and late apoptotic cells were increased significantly relative to that of untreated control cells in dose-dependent manner.

Cell Cycle Analysis^[1]

Cell Line:	HT-29
Concentration:	0, 1, 5, and 10 µM
Incubation Time:	48 h
Result:	Increased the population of cells in sub G1 and G0/G1 phase and decreased the population of cells in S phase.

分子量

345.39

Formula

C₂₁H₁₉N₃O₂

CAS 号

2456315-41-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Azimian F, et al. Synthesis and biological evaluation of diaryl urea derivatives designed as potential anticarcinoma agents using de novo structure-based lead optimization approach. Eur J Med Chem. 2020 Sep 1;201:112461.

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VEGFR-2-IN-13

发表于2024年12月3日由上海金畔生物科技有限公司

VEGFR-2-IN-13

VEGFR-2-IN-13 (Compound 19a) 是一种有效的 VEGFR-2 抑制剂，IC₅₀ 为 3.4 nM。VEGFR-2-IN-13 阻滞 HepG2 细胞周期的 G2/M 期，诱导细胞凋亡 (apoptosis)。

VEGFR-2-IN-13 Chemical Structure

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生物活性

VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor with an IC₅₀ of 3.4 nM. VEGFR-2-IN-13 disrupts the HepG2 cell cycle by arresting the G2/M phase and induces apoptosis^[1].

IC₅₀ & Target

VEGFR2

3.4 nM (IC₅₀)

体外研究
(In Vitro)

VEGFR-2-IN-13 (Compound 19a) shows anti-proliferative activities with IC₅₀ values of 8.2 µM and 5.4 µM against MCF-7 and HepG2 cells, respectively^[1].

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

分子量

454.50

Formula

C₂₄H₁₈N₆O₂S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Alsaif NA, et al. Identification of new [1,2,4]triazolo[4,3-a]quinoxalines as potent VEGFR-2 tyrosine kinase inhibitors: Design, synthesis, anticancer evaluation, and in silico studies. Bioorg Med Chem. 2021 Sep 15;46:116384.

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VEGFR-2-IN-17

发表于2024年12月3日由上海金畔生物科技有限公司

VEGFR-2-IN-17

VEGFR-2-IN-17 (Compound 15a) 是一种有效的 VEGFR-2 抑制剂，IC₅₀ 值为 67.25 nM。VEGFR-2-IN-17 具有抗肿瘤活性。

VEGFR-2-IN-17 Chemical Structure

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生物活性

VEGFR-2-IN-17 (Compound 15a) is a potent VEGFR-2 inhibitor with an IC₅₀ of 67.25 nM. VEGFR-2-IN-17 shows antitumor activities^[1].

IC₅₀ & Target

VEGFR2

67.25 nM (IC₅₀)

体外研究
(In Vitro)

VEGFR-2-IN-17 (Compound 15a) shows antiproliferative activities with IC₅₀ values of 34.59 ± 2.82, 30.28 ± 2.56, 47.10 ± 3.59 and 250.33 ± 2.51 µM against HepG2, PC3, MCF-7 and WI-38 cells, respectively^[1].

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

分子量

375.81

Formula

C₂₁H₁₄ClN₃O₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Abdallah AE, et al. Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors. J Enzyme Inhib Med Chem. 2022 Dec;37(1):573-591.

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VEGFR-2-IN-15

发表于2024年12月3日由上海金畔生物科技有限公司

VEGFR-2-IN-15

VEGFR-2-IN-15 (Compound 14b) 是一种有效的 VEGFR-2 抑制剂。VEGFR-2-IN-15 抑制 HepG2 细胞在 Pre-G1 期的生长，诱导细胞凋亡 (apoptosis)。

VEGFR-2-IN-15 Chemical Structure

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生物活性

VEGFR-2-IN-15 (Compound 14b) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-15 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis^[1].

IC₅₀ & Target

VEGFR2

体外研究
(In Vitro)

VEGFR-2-IN-15 (Compound 14b) shows cytotoxic activities with IC₅₀ values of 4.754 ± 0.21 µM and 4.61 ± 0.34 µM against MCF-7 and HepG2 cells, respectively^[1].
VEGFR-2-IN-15 shows the highest activities with VEGFR-2 protein concentrations of 705.7 pg/ml^[1].

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

分子量

467.92

Formula

C₂₃H₁₈ClN₃O₄S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Elkady H, et al. New benzoxazole derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative evaluation, flowcytometric analysis, and in silico studies. J Enzyme Inhib Med Chem. 2022 Dec;37(1):397-410.

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VEGFR-2-IN-14

发表于2024年12月2日由上海金畔生物科技有限公司

VEGFR-2-IN-14

VEGFR-2-IN-14 (Compound 5) 是一种有效的 VEGFR-2 抑制剂。VEGFR-2-IN-14 抑制 HepG2 细胞在 Pre-G1 期的生长，诱导细胞凋亡 (apoptosis)。

VEGFR-2-IN-14 Chemical Structure

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生物活性

VEGFR-2-IN-14 (Compound 5) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-14 arrests the HepG2 cell growth at the Pre-G1 phase and induces apoptosis^[1].

IC₅₀ & Target

VEGFR2

体外研究
(In Vitro)

VEGFR-2-IN-14 (Compound 5) shows cytotoxic activities with IC₅₀ values of 9.7 ± 0.75 µM and 8.8 ± 0.69 µM against MCF-7 and HepG2 cells, respectively^[1].
VEGFR-2-IN-14 shows VEGFR-2 inhibitory effects with concentrations of 610.4 pg/ml^[1].

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

分子量

433.52

Formula

C₂₄H₂₃N₃O₃S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Hagras M, et al. 1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and in silico studies. J Enzyme Inhib Med Chem. 2022 Dec;37(1):380-396.

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VEGFR-2-IN-18

发表于2024年12月2日由上海金畔生物科技有限公司

VEGFR-2-IN-18

VEGFR-2-IN-18 (Compound 15d) 是一种有效的 VEGFR-2 抑制剂，IC₅₀ 值为 60 nM。VEGFR-2-IN-18 诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。

VEGFR-2-IN-18 Chemical Structure

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生物活性

VEGFR-2-IN-18 (Compound 15d) is a potent VEGFR-2 inhibitor with an IC₅₀ of 60 nM. VEGFR-2-IN-18 induces cell apoptosis. VEGFR-2-IN-18 shows antitumor activities^[1].

IC₅₀ & Target

VEGFR2

60 nM (IC₅₀)

体外研究
(In Vitro)

VEGFR-2-IN-18 (Compound 15d) shows antiproliferative activities with IC₅₀ values of 24.10 ± 2.12, 40.90 ± 3.46, 33.40 ± 2.92 and 221.25 ± 2.55 µM against HepG2, PC3, MCF-7 and WI-38 cells, respectively^[1].

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

分子量

376.80

Formula

C₂₀H₁₃ClN₄O₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Abdallah AE, et al. Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors. J Enzyme Inhib Med Chem. 2022 Dec;37(1):573-591.

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VEGFR-2-IN-16

发表于2024年12月2日由上海金畔生物科技有限公司

VEGFR-2-IN-16

VEGFR-2-IN-16 (Compound 15b) 是一种有效的 VEGFR-2 抑制剂，IC₅₀ 值为 86.36 nM。VEGFR-2-IN-16 具有抗肿瘤活性。

VEGFR-2-IN-16 Chemical Structure

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生物活性

VEGFR-2-IN-16 (Compound 15b) is a potent VEGFR-2 inhibitor with an IC₅₀ of 86.36 nM. VEGFR-2-IN-16 shows antitumor activities^[1].

IC₅₀ & Target

VEGFR2

86.36 nM (IC₅₀)

体外研究
(In Vitro)

VEGFR-2-IN-16 (Compound 15b) shows antiproliferative activities with IC₅₀ values of 17.39 ± 1.54, 25.58 ± 2.31, 19.88 ± 1.79 and 233.21 ± 2.39 µM against HepG2, PC3, MCF-7 and WI-38 cells, respectively^[1].

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

分子量

410.25

Formula

C₂₁H₁₃Cl₂N₃O₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Abdallah AE, et al. Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors. J Enzyme Inhib Med Chem. 2022 Dec;37(1):573-591.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

VEGFR-2/BRAF-IN-1

发表于2024年12月1日由上海金畔生物科技有限公司

VEGFR-2/BRAF-IN-1

VEGFR-2/BRAF-IN-1 (Compound 4b) 是一种 VEGFR-2 和 BRAF 双重抑制剂，对 VEGFR-2、BRAF^V600E 和 BRAF^WT 的 IC₅₀ 分别为 0.049、0.063 和 0.005 µM。VEGFR-2/BRAF-IN-1 诱导细胞凋亡，在 G1/S 期阻滞细胞周期。

VEGFR-2/BRAF-IN-1 Chemical Structure

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生物活性

VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC₅₀ values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF^V600E and BRAF^WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase^[1].

IC₅₀ & Target

VEGFR2

0.049 μM (IC₅₀)

BRaf^V600E

0.063 μM (IC₅₀)

BRAF^WT

0.005 μM (IC₅₀)

分子量

642.50

Formula

C₂₆H₂₀Cl₂F₃N₅O₃S₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Hassan RA, et al. Novel antiproliferative agents bearing substituted thieno[2,3-d]pyrimidine scaffold as dual VEGFR-2 and BRAF kinases inhibitors and apoptosis inducers; design, synthesis and molecular docking. Bioorg Chem. 2022 May 10;125:105861.

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VEGFR-2/BRAF-IN-2

发表于2024年12月1日由上海金畔生物科技有限公司

VEGFR-2/BRAF-IN-2

VEGFR-2/BRAF-IN-2 (Compound 4a) 是一种 VEGFR-2 和 BRAF 双重抑制剂，对 VEGFR-2、BRAF^V600E、BRAF^WT 的 IC₅₀ 分别为 0.111、0.089 和 0.071 µM。VEGFR-2/BRAF-IN-2 诱导细胞凋亡，在 G1 期阻滞细胞周期。

VEGFR-2/BRAF-IN-2 Chemical Structure

规格		是否有货
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生物活性

VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC₅₀ values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF^V600E and BRAF^WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase^[1].

IC₅₀ & Target

VEGFR2

0.111 μM (IC₅₀)

BRaf^V600E

0.089 μM (IC₅₀)

BRAF^WT

0.071 μM (IC₅₀)

分子量

608.05

Formula

C₂₆H₂₁ClF₃N₅O₃S₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Hassan RA, et al. Novel antiproliferative agents bearing substituted thieno[2,3-d]pyrimidine scaffold as dual VEGFR-2 and BRAF kinases inhibitors and apoptosis inducers; design, synthesis and molecular docking. Bioorg Chem. 2022 May 10;125:105861.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

VEGFR2-IN-1

发表于2024年11月28日由上海金畔生物科技有限公司

VEGFR2-IN-1

VEGFR2-IN-1 是一种有效的选择性 VEGFR2 抑制剂 (IC₅₀=19.8 nM)。VEGFR2-IN-1 通过凋亡激活和抑制 VEGFR2 的表达来抑制细胞的增殖和迁移。

VEGFR2-IN-1 Chemical Structure

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生物活性

VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC₅₀=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition^[1].

IC₅₀ & Target

VEGFR2

19.8 nM (IC₅₀)

体外研究
(In Vitro)

VEGFR2-IN-1 (compound 17; 0.1, 1, 10, 100 μM; 48 hours) shows an effective and selective agent against MCF-7 (IC₅₀=1.18 μM), MDA-MB-231 (IC₅₀=10.49 μM), MCF-10A (IC₅₀=24.76 μM) cells^[1]. VEGFR2-IN-1 (MCF-7 cells; 48 hours) induces cell cycle arrest at the G1 and S-phases^[1]. VEGFR2-IN-1 (MCF-7 cells) shows the upregulation of pro-apoptotic genes (p53, Bax, caspases-3, caspases-9) and downregulation of antiapoptotic gene (Bcl-2)^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:	MCF-7, MDA-MB-231, MCF-10A cells
Concentration:	0.1, 1, 10, 100 μM
Incubation Time:	48 hours
Result:	Exhibited an effective and selective agent against MCF-7 (IC₅₀=1.18 μM), MDA-MB-231 (IC₅₀=10.49 μM), MCF-10A (IC₅₀=24.76 μM) cells.

体内研究
(In Vivo)

VEGFR2-IN-1 (4.2 mg/kg; i.p.; once a day for 7 days) shows anticancer activity with an improvement of hematological, biochemical parameters^[1]. Animal Model: Male Swiss albino mice, 21-28 g (Xenograft model)^[1].

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

Animal Model:	Male Swiss albino mice, 21-28 g (Xenograft model)^[1]
Dosage:	4.2 mg/kg
Administration:	i.p.; once a days; 7 days
Result:	Showed anticancer activity by having a tumor inhibition ratio of 54.2% with an improvement of hematological, biochemical parameters.

分子量

398.48

Formula

C₂₂H₁₈N₆S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献

[1]. Nafie MS, Boraei ATA. Exploration of novel VEGFR2 tyrosine kinase inhibitors via design and synthesis of new alkylated indolyl-triazole Schiff bases for targeting breast cancer. Bioorg Chem. 2022; 122:105708.

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whatman (沃特曼)

英国沃特曼 Millipore PALL中国代理商金畔官网

标签归档：vegfr

TIE-2/VEGFR-2 kinase-IN-2

TIE-2/VEGFR-2 kinase-IN-2

TIE-2/VEGFR-2 kinase-IN-2

VEGFR-2-IN-20

VEGFR-2-IN-10

VEGFR-2-IN-10

VEGFR-2-IN-10

VEGFR-IN-1

VEGFR-IN-1

VEGFR-IN-1

VEGFR-2-IN-19

VEGFR-2-IN-13

VEGFR-2-IN-17

VEGFR-2-IN-15

VEGFR-2-IN-14

VEGFR-2-IN-18

VEGFR-2-IN-16

VEGFR-2/BRAF-IN-1

VEGFR-2/BRAF-IN-2

VEGFR2-IN-1