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Aflibercept (Synonyms: VEGF Trap; VEGF-TRAPR1R2; VEGF-trapR1)

رقم الكتالوجGC68628

أفليبرسبت (VEGF Trap) هو مستحضر يتكون من نطاقات Ig لمستقبلات VEGFR1 و VEGFR2 المذابة في الجزء الخارجي للخلايا، والتي تم دمجها مع Fc المصنوع من IgG1 البشرية. يعمل أفليبرسبت على تثبيط إشارات VEGF عن طريق قمع المسارات التي يشارك فيها VEGF في التحكم. يُستخدَم أفليبرسبت في دراسة تغير شبكية العين المرتبط بالشِّـــــــ َّ ْٔ خِلاَّصِّ ُولِى، وأمراض القلب والأوعية الدَّمَوِية.

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Aflibercept التركيب الكيميائي

Cas No.: 862111-32-8

الحجم السعر المخزون الكميّة
500ug
340٫00
متوفر
1mg
546٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of Aflibercept

Aflibercept is a high-affinity soluble decoy vascular endothelial growth factor (VEGF) receptor and a potent angiogenesis inhibitor that binds vascular endothelial growth factor and placental growth factor (PlGF) with extremely high affinity. Preclinical studies have shown that Aflibercept has potent antitumor and antiangiogenic activities against a variety of tumors, including melanoma and solid tumors[1].

Aflibercept (7.5μg/ml; 10min) inhibits galectin-1-mediated VEGFR2 activation[2]. Aflibercept (15nM; 1h) does not exhibit significant cell surface binding to ARPE-19 and HUVEC. Aflibercept (500nM; 10-15min) in the presence of heparin was unable to stimulate serotonin release[3].

Aflibercept (10 and 25mg/kg; SC; twice-weekly; 30 days) inhibited primary tumor growth by 74% and 78% and Formation of detectable lung metastases was inhibited in 98% of cases [4] . Aflibercept (10mg/kg; 3h) can reduce stroke-induced VEGF-A and VEGFR2 expression, alleviate brain edema and Blood-Brain Barrier disruption, and improve the survival rate of obese mice after stroke after middle cerebral artery occlusion (MCAO) [5].

References:
[1] Bender J G, Blaney S M, Borinstein S, et al. A phase I trial and pharmacokinetic study of aflibercept (VEGF Trap) in children with refractory solid tumors: a children's oncology group phase I consortium report[J]. Clinical cancer research, 2012, 18(18): 5081-5089.
[2] Kanda A, Noda K, Saito W, Ishida S. Aflibercept Traps Galectin-1, an Angiogenic Factor Associated with Diabetic Retinopathy. Sci Rep. 2015 Dec 9;5:17946.
[3] MacDonald DA, Martin J, Muthusamy KK, Luo JK, Pyles E, Rafique A, Huang T, Potocky T, Liu Y, Cao J, Bono F, Delesque N, Savi P, Francis J, Amirkhosravi A, Meyer T, Romano C, Glinka M, Yancopoulos GD, Stahl N, Wiegand SJ, Papadopoulos N. Aflibercept exhibits VEGF binding stoichiometry distinct from bevacizumab and does not support formation of immune-like complexes. Angiogenesis. 2016 Jul;19(3):389-406.
[4] Moroney JW, Sood AK, Coleman RL. Aflibercept in epithelial ovarian carcinoma. Future Oncol. 2009 Jun;5(5):591-600.
[5] Kim ID, Cave JW, Cho S. Aflibercept, a VEGF (Vascular Endothelial Growth Factor)-Trap, Reduces Vascular Permeability and Stroke-Induced Brain Swelling in Obese Mice. Stroke. 2021 Aug;52(8):2637-2648.

Protocol of Aflibercept

Cell experiment [1]:

Cell lines

Human RPE (hTERT-RPE1) cells

Preparation Method

Human RPE (hTERT-RPE1) cells were treated with Aflibercept (7.5μg/ml) for 10min.

Reaction Conditions

Aflibercept: 7.5μg/ml; 10min

Applications

Aflibercept (7.5μg/ml; 10min) inhibits galectin-1-mediated VEGFR2 activation.
Animal experiment [2]:

Animal models

Orthotopic murine renal cancer cell model

Preparation Method

Aflibercept 10 and 25mg/kg versus solvents control was administered subcutaneously twice-weekly for up to 30 days. 

Dosage form

10 and 25mg/kg; SC; twice-weekly; 30d

Applications

Aflibercept (10 and 25mg/kg; SC; twice-weekly; 30d) inhibited primary tumor growth by 74% and 78% and Formation of detectable lung metastases was inhibited in 98% of cases.

References:
[1] Kanda A, Noda K, Saito W, Ishida S. Aflibercept Traps Galectin-1, an Angiogenic Factor Associated with Diabetic Retinopathy. Sci Rep. 2015 Dec 9;5:17946.
[2] Moroney JW, Sood AK, Coleman RL. Aflibercept in epithelial ovarian carcinoma. Future Oncol. 2009 Jun;5(5):591-600.

Chemical Properties of Aflibercept

Cas No. 862111-32-8 SDF
المرادفات VEGF Trap; VEGF-TRAPR1R2; VEGF-trapR1
Formula M.Wt
الذوبان Storage Sealed and stored at ≤ -30°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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