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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Cas No.: 862111-32-8
Sample solution is provided at 25 µL, 10mM.
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.
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: |
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. |
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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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