Cabozantinib hydrochloride(Synonyms: XL184 hydrochloride; BMS-907351 hydrochloride)

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Cabozantinib hydrochloride (Synonyms: XL184 hydrochloride; BMS-907351 hydrochloride)

Cabozantinib hydrochloride 是一种口服有效的 VEGFR2 和 MET 抑制剂，IC50 分别为 0.035 和 1.3 nM。Cabozantinib hydrochloride 对 KIT、RET、AXL、TIE2 和 FLT3 有较强的抑制作用 (IC50=4.6、5.2、7、14.3 和 11.3 nM)。Cabozantinib hydrochloride 显示出抗血管生成活性。Cabozantinib hydrochloride 可以破坏肿瘤血管，促进肿瘤和内皮细胞凋亡 (apoptosis)。

Cabozantinib hydrochloride(Synonyms: XL184 hydrochloride; BMS-907351 hydrochloride)

Cabozantinib hydrochloride Chemical Structure

CAS No. : 1817759-42-4

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Cabozantinib hydrochloride 的其他形式现货产品:

Cabozantinib

生物活性

Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[1].

IC50 & Target

VEGFR2

0.035 ± 0. nM (IC50)

MET

1.3 ± 1.2 nM (IC50)

METY1248H

3.8 nM (IC50)

METD1246N

11.8 nM (IC50)

Flt-4

6 nM (IC50)

Flt-1

12 nM (IC50)

体外研究
(In Vitro)

Cabozantinib hydrochloride inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively[1].
Cabozantinib hydrochloride (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50 values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively[1].
Cabozantinib hydrochloride (0-370 nM, 24 h) inhibits cellular migration and invasion[1].
Cabozantinib hydrochloride (48 h) inhibits tumor cell proliferation in a variety of tumor types[1].

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

Cell Proliferation Assay

Cell Line: SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells[1]
Concentration:
Incubation Time: 48 hours
Result: Inhibited tumor cell proliferation, with IC50 of 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200, and 10800 nM, respectively.

Cell Migration Assay

Cell Line: B16F10 cells[1]
Concentration: 0, 41, 123, and 370 nM
Incubation Time: 24 hours
Result: Potently inhibited HGF-induced migration (IC50 = 31 nM) of B16F10 cells.

Cell Invasion Assay

Cell Line: B16F10 cells[1]
Concentration: 0, 1.5, 14, and 123 nM
Incubation Time: 24 hours
Result: Potently inhibited HGF-induced invasion (IC50 = 9 nM) of B16F10 cells.

体内研究
(In Vivo)

Cabozantinib hydrochloride (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice[1].
Cabozantinib hydrochloride (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis[1].
Cabozantinib hydrochloride (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner[1].

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

Animal Model: Female mice bearing MBA-MB-231 tumor (5 per group)[1]
Dosage: 0, 100 mg/kg
Administration: Orally, once
Result: Inhibited MET and VEGFR2 phosphorylation.
Animal Model: Mice bearing MBA-MB-231 tumor[1]
Dosage: 1, 3, 10, 30, 60 mg/kg
Administration: Orally, once daily for 14 days
Result: Inhibited tumor growth in a dose-dependent manner.

分子量

537.97

Formula

C28H25ClFN3O5
CAS 号

1817759-42-4
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]. 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]. 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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