Cabozantinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cabozantinib (XL184, BMS-907351) 是一种有效的多激酶抑制剂，可抑制 VEGFR2、c-Met、Kit、Axl 和 Flt3，IC50 分别为 0.035、1.3、4.6、7 和 11.3 nM。

Cabozantinib (XL184, BMS-907351) is a potent multi-kinase inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50 of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively; eliminates tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and tumor cell apoptosis, and slows regrowth of the tumor vasculature, also decreases invasiveness of primary tumors and reduces metastasis in pancreatic islet cancer; exerts marked anti-MPNST effects in vitro and in vivo.Kidney Cancer Approved(In Vitro):Cabozantinib 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.Cabozantinib (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.Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion.Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types.(In Vivo):Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice.Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis.Cabozantinib (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner.

Cabozantinib 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.Cabozantinib (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.Cabozantinib (0-370 nM, 24 h) inhibits cellular migration and invasion.Cabozantinib (48 h) inhibits tumor cell proliferation in a variety of tumor types. Cell Proliferation Assay Cell Line:SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells 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 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 Concentration:0, 1.5, 14, and 123 nM Incubation Time:24 hours Result:Potently inhibited HGF-induced invasion (IC50 = 9 nM) of B16F10 cells.

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

XL184 | BMS-907351 | XL-184 | XL184

Angiogenesis

VEGFR

AXL|c-Met|Kit|VEGFR2/KDR|VEGFR3/FLT4|VEGFR2|MET|MET(Y1248H)|RET|FLT3

Cancer

Kidney Cancer

849217-68-1

501.5057

C28H24FN3O5

>98% (HPLC)

DMSO: ≥ 30 mg/mL

COC1=CC2=NC=CC(OC3=CC=C(C=C3)N(C(=O)C3(CC3)C(N)=O)C3=CC=C(F)C=C3)=C2C=C1OC

1,1-Cyclopropanedicarboxamide, N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N-(4-fluorophenyl)-

(-20℃)

With Ice Pack

≥ 2 years