货号	规格	价格	上海	北京	珠海	重庆	武汉
S81149-5mg买3赠1	99.80%	￥232.00 S81149-5mg ￥232.00 现货（买3赠1）	3 3	-	-	-	-
S81149-10mg买3赠1	99.80%	￥320.00 S81149-10mg ￥320.00 现货（买3赠1）	3 3	-	-	-	-
S81149-25mg买3赠1	99.80%	￥560.00 S81149-25mg ￥560.00 现货（买3赠1）	2 2	-	-	-	-
S81149-50mg买3赠1	99.80%	￥1040.00 S81149-50mg ￥1040.00 现货（买3赠1）	4 4	-	-	-	-
S81149-100mg买3赠1	99.80%	￥1760.00 S81149-100mg ￥1760.00 现货（买3赠1）	2 2	-	-	-	-
S81149-200mg买3赠1	≥98%	￥2480.00 S81149-200mg ￥2480.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively

靶点：

EGFR2：1.5 nM (IC50)；PDGFRα：1.1 nM (IC50)；FGFR1：2.2 nM (IC50)；c-Kit：12.5 nM (IC50);VEGFR; FGFR; Bcr-Abl; PDGFR; Src; c-Kit; Autophagy

体内研究：

In a survival model in which mice are instead injected with Ba/F3 BCR-ABLT315I cells, administration of Dasatinib at doses as high as 300 mg/kg has no effect on survival time. By contrast, treatment with Ponatinib (AP24534) prolongs survival in a dose-dependent manner. Ponatinib dosed orally for 19 days at 5, 15, and 25 mg/kg prolongs median survival to 19.5, 26, and 30 days, respectively compare to 16 days for vehicle-treated mice (p<0.01 for all three dose levels). The anti-tumor activity of Ponatinib (AP24534) is further assessed in a xenograft model in which Ba/F3 BCR-ABLT315I cells are injected subcutaneously into mice. Tumor growth is inhibited by Ponatinib in a dose-dependent manner compare to vehicle-treated mice, with significant suppression of tumor growth upon daily oral dosing at 10 and 30 mg/kg (%T/C = 68% and 20%, respectively; p<0.01 for both dose levels). Daily oral dosing of 50 mg/kg Ponatinib causes significant tumor regression (%T/C = 0.9%, p<0.01), with a 96% reduction in mean tumor volume at the final measurement compared to the start of treatment. Ponatinib is well tolerated at all efficacious dose levels for the duration of the study; maximal decreases in body weight are <5%, <5%, and <12% for the 10, 30, and 50 mg/kg dose groups, respectively, with no signs of overt toxicity Ponatinib (1-25 mg/kg) is administered orally, once daily for 28 days, to mice bearing MV4-11 xenografts. Ponatinib potently inhibits tumor growth in a dose-dependent manner. Administration of 1 mg/kg, t

参考文献：

1. O'Hare T, et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell, 2009, 16(5), 401-412。 2. Gozgit JM, et al. Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol Cancer Ther, 2011, 10(6), 1028-1035. 3. Uchida T, et al. Hes1 upregulation contributes to the development of FIP1L1-PDGRA-positive leukemia in blast crisis. Exp Hematol. 2014 May;42(5):369-379.e3.

溶解性：

1M HCl : 50 mg/mL (93.89 mM; ultrasonic and adjust pH to 1 with HCl) DMSO : 50 mg/mL (93.89 mM; Need ultrasonic)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.878 ml	9.388 ml	18.777 ml
5 mM	0.376 ml	1.878 ml	3.755 ml
10 mM	0.188 ml	0.939 ml	1.878 ml
50 mM	0.038 ml	0.188 ml	0.376 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献(3篇)

3. [IF=6.9] Xingyue He et al."APMCG-1 attenuates ischemic stroke injury by reducing oxidative stress and apoptosis and promoting angiogenesis via activating PI3K/AKT pathway."BIOMEDICINE & PHARMACOTHERAPY.2024 Nov;180:117506 2. [IF=4.7] Yule Wang et al."Guanxinning Tablet Alleviates Post-Ischemic Stroke Injury Via Regulating Complement and Coagulation Cascades Pathway and Inflammatory Network Mobilization."Drug Design Development and Therapy. 1. [IF=7.419] Yule Wang et al."Discovery of anti-stroke active substances in Guhong injection based on multi-phenotypic screening of zebrafish."BIOMEDICINE & PHARMACOTHERAPY.2022 Nov;155:113744

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