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Cabozantinib hydrochloride

Cabozantinib hydrochloride

产品编号 T5164   CAS 1817759-42-4
别名: XL184, Cabozantinib hydrochloride (849217-68-1(free base)), BMS-907351, 盐酸卡博替尼

Cabozantinib hydrochloride (XL184) 是一种有效的泛酪氨酸激酶抑制剂,可抑制 VEGFR2、c-Met、Kit、Axl 和 Flt4(IC50:0.035、1.3、4.6、7 和 6 nM)。

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Cabozantinib hydrochloride Chemical Structure
Cabozantinib hydrochloride, CAS 1817759-42-4
规格 价格/CNY 货期 数量
1 mg ¥ 248 现货
2 mg ¥ 350 现货
5 mg ¥ 620 现货
10 mg ¥ 960 现货
25 mg ¥ 1,670 现货
50 mg ¥ 2,520 现货
100 mg ¥ 3,560 现货
200 mg ¥ 5,130 现货
500 mg ¥ 7,860 现货
其他形式的 Cabozantinib hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
产品目录号及名称: Cabozantinib hydrochloride (T5164)
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纯度: 97.09%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).
靶点活性 RORγ:111 nM (Ki), RORα:172 nM (Ki)
体外活性 SR1001 binds specifically to the ligand-binding domains of RORα and RORγt, inducing a conformational change within the ligand-binding domain, resulting in suppression of the receptors' transcriptional activity. SR1001 inhibited the development of murine T(H)17 cells. Furthermore, SR1001 inhibited the expression of cytokines when added to differentiated murine or human T(H)17 cells [1]. Treatment with the RORγT inhibitor SR1001 to abrogate Th17 cell function reduced Th17-dependent learned helplessness [2].
体内活性 After myelin oligodendrocyte glycoprotein (MOG35–55) immunization at day 0, experimental autoimmune encephalomyelitis (EAE) mice were treated with SR1001 (25 mg/kg, b.i.d. i.p.) for the duration of the study. Further analysis of spinal cords from mice harvested at day 18 post-immunization revealed that SR1001 repressed Il17a mRNA expression by ~60%, as well as reduced Il21, and Il22 mRNA expression [1]. When these mice were injected with SR1001, the circadian rhythm of CS expression was eliminated [3].
细胞实验 CD4+ T cells were isolated as described previously and in the Supplementary Materials. CD4+ T cells cultured with splenic feeder cells were activated with 2.5 μg/mL of anti-CD3 (clone 145–11), and differentiated to Th17 cells by addition of IL-6 (20 ng/mL; Peprotech), TGFβ (5 ng/mL), anti-IL-4 (10 μg/mL; clone 11B11, UAB core facility) and anti-IFNγ (10 μg/mL; clone XMG1.2, UAB core facility). After 5 days of differentiation toward Th17 cells, cells were recovered after histopaque gradient purification and resuspended in PBS. An aliquot of cells was used to evaluate the percent of Th17 cells (~40%) and ~10–20×106 undifferentiated CD4+ T or Th17 cells were injected in 500 μL PBS by tail vein 48 h prior to behavioral testing. Where indicated, mice were injected intraperitoneally with 100 μg anti-IL-17A, or 125 μg SR1001 daily beginning 1 day before Th17 cell transfer, and this was continued throughout the experiment. As controls, mice were injected i.v. with ~10–20×106 CD4+ T cells to evaluate the effect of non-differentiated cells, or with 500 μL PBS to mimic the stress of tail vein i.v. injection 48 h prior to behavioral testing. Intracellular cytokine staining was carried out as described previously and in the Supplementary Information [2].
动物实验 For circadian gene expression experiments male C57BL6 mice (8–10 weeks of age) were either maintained on a L:D (12h∶12h) cycle or on constant darkness (1 day). At the circadian time (CT) 0 animals were administered a single dose of 25 mg/kg SR1001 (i.p.) and groups of animals (n?=?6) were sacrificed at CT0, CT6, CT12, and CT18. Gene expression was determined by real-time qPCR. Gene expression was normalized to Cyclophin b in all experiments [3].
别名 XL184, Cabozantinib hydrochloride (849217-68-1(free base)), BMS-907351, 盐酸卡博替尼
分子量 537.96
分子式 C28H25ClFN3O5
CAS No. 1817759-42-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 80 mg/mL

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TargetMol Library Books参考文献

1. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308. 2. Torres KE, et al. Activated MET is a molecular prognosticator and potential therapeutic target for malignant peripheral nerve sheath tumors.Clin Cancer Res. 2011 Jun 15;17(12):3943-55. 3. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768.
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相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抗癌药物库 EMA 上市药物库 抗癌临床化合物库 抗癌活性化合物库 抗癌上市药物库 药物功能重定位化合物库 抑制剂库 已知活性化合物库 抗前列腺癌化合物库

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Cabozantinib hydrochloride 1817759-42-4 Angiogenesis Metabolism Tyrosine Kinase/Adaptors VEGFR FLT c-Met/HGFR TAM Receptor c-Kit ROR inhibit CD135 Mer Fms like tyrosine kinase 3 Inhibitor XL184 SCFR BMS 907351 Axl XL 184 Cluster of differentiation antigen 135 XL-184 Vascular endothelial growth factor receptor Cabozantinib hydrochloride (849217-68-1(free base)) angiogenesis CD117 BMS-907351 BMS907351 FLT3 HT1080 Cabozantinib Hydrochloride A431 antiangiogenic Apoptosis Tyro3 Cabozantinib 盐酸卡博替尼 B16F10 cells inhibitor

 

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