Cabozantinib (XL184, BMS-907351)

Cabozantinib (XL184, BMS-907351)は一種の有効なVEGFR2阻害剤で、無細胞試験でIC50値が0.035 nMです。Cabozantinib (XL184, BMS-907351)はc-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXLに有効に作用する時のIC50値が1.3 nM,4 nM,4.6 nM,12 nM/11.3 nM/6 nM,14.3 nM 和 7 nMにそれぞれ分かれます。

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Cabozantinib (XL184, BMS-907351) 化学構造
分子量: 501.51

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製品説明

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製品の説明

生物活性

製品説明 Cabozantinib (XL184, BMS-907351)は一種の有効なVEGFR2阻害剤で、無細胞試験でIC50値が0.035 nMです。Cabozantinib (XL184, BMS-907351)はc-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXLに有効に作用する時のIC50値が1.3 nM,4 nM,4.6 nM,12 nM/11.3 nM/6 nM,14.3 nM 和 7 nMにそれぞれ分かれます。
ターゲット

VEGFR2

c-Met Ret c-Kit Flt-1/3/4 Tie2
IC50 0.035 nM 1.3 nM 4 nM 4.6 nM 12 nM/11.3 nM/6 nM 14.3 nM [1]
In vitro試験 XL184 has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. [1] XL184 at low concentration (0.1-0.5 μM) is sufficient to induce marked inhibition of constitutive and inducible Met phosphorylation and its resultant downstream signaling in MPNST cells, and inhibit HGF-induced MPNST cell migration and invasion. XL184 also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although XL-184 has no significant effect on MPNST cell growth at 0.1 μM, XL184 at 5-10 μM significantly inhibits the MPNST cell growth. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
E98NT  NFKxNIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfD[ZMxNjBzLUGwJO69VQ>? M1jRWGROW09? M2TSZWlEPTB;OEmgcm0> MmezNlM1QDRyME[=
SNU-5  NYq5T5ZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoO4TWM2OD1iMUmgcm0> MUmyNVkzPjF7MR?=
Hs746T  NIHTbGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPRTWM2OD17Lkmgcm0> NVXoe|JKOjF7Mk[xPVE>
SNU-1  MoTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\wdWlEPTB;NUKyN{BvVQ>? NXzQU4hVOjF7Mk[xPVE>
SNU-16 NXTTZWFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XpSWlEPTB;MUG0PUBvVQ>? NV3JWINYOjF7Mk[xPVE>
MDA-MB-231 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrTU4tKSzVyPTC2OFIyKG6P NEjHNlMzOTl{NkG5NS=>
U87MG NVj3XYJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4r3UGlEPTB;MUi1NUBvVQ>? NFrJOlczOTl{NkG5NS=>
H441  NGLKN|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVq5RpNDUUN3ME2yNVcxOCCwTR?= NYrKWYxtOjF7Mk[xPVE>
H69 M323NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPpcFA5UUN3ME2yNFIxOCCwTR?= NE\EN3kzOTl{NkG5NS=>
PC3 NHjMfZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTFyOECwJI5O NWfBelJYOjF7Mk[xPVE>
MTC-TT MlL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3vdlhKSzVyPUCuNFQhMyByLkCzJO69VQ>? Mn;mNlE1PzB7OUW=
MZ-CRC MmfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTZTWM2OD5iNTFOwG0> M33jVVIyPDdyOUm1
TPC-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3i0VmlEPTB;MD6wOkAsKDBwMEKg{txO M363PVIyPDdyOUm1

... Click to View More Cell Line Experimental Data

In vivo試験 XL184 treatment at 30 mg/kg in RIP-Tag2 mice with spontaneous pancreatic islet tumors disrupts 83% of the tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and extensive tumor cell apoptosis, and slows regrowth of the tumor vasculature after drug withdrawal, more significantly compared with XL999 that blocks VEGFR but not c-Met, leading to only 43% reduction in vascularity, suggesting that concurrent inhibition of VEGFR and other functionally relevant receptor tyrosine kinases (RTK) amplifies angiogenesis inhibition. XL184 also decreases invasiveness of primary tumors and reduces metastasis. [1] XL184 at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. [2] Administration of XL184 induces dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models, in association with decreased tumor and endothelial cell proliferation as well as increased apoptosis. A single oral dose of XL184 is sufficient to induce sustained tumor growth inhibition in MDA-MB-231 tumor-bearing mice and C6 tumor-bearing rats at 100 mg/kg and 10 mg/kg, respectively. [3]
臨床試験 XL184 is currently under Phase III study versus mitoxantrone plus prednisone in men with previously treated symptomatic castration-resistant prostate cancer (COMET-2).
特集

プロトコル (参考用のみ)

細胞アッセイ:

[2]

細胞株 ST88-14, STS26T, and MPNST724
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 48 hours
実験の流れ

Cells are exposed to various concentrations of XL184 for 48 hours. Cell growth is determined by MTS assays using CellTiter96 Aqueous Non-Radioactive Cell Proliferation Assay kit. Absorbance is measured at a wavelength of 490 nm, and the absorbance values of treated cells are presented as a percentage of the absorbance of untreated cells.

動物実験:

[1]

動物モデル RIP-Tag2 transgenic mice in a C57BL/6 background with spontaneous pancreatic islet tumors
製剤 Suspended at a concentration of 5 mg/mL in sterile saline or water
投薬量 ~60 mg/kg
投与方法 Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Cabozantinib (XL184, BMS-907351) SDF
分子量 501.51
化学式

C28H24FN3O5

CAS No. 849217-68-1
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL (199.39 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

文献中の引用 (13)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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