Cabozantinib | XL184;BMS-907351 | c-Met/HGFR | FLT3 | VEGFR | c-Kit | Tie-2

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卡博替尼 /Cabozantinib {[allProObj[0].p_purity_real_show]}

货号：A200488 同义名： XL184;BMS-907351

Cabozantinib是一种强效和口服活性的 VEGFR2 和 MET 抑制剂，IC50 值分别为 0.035 和 1.3 nM。它还强效抑制 KIT、RET、AXL、TIE2 和 FLT3，IC50 值分别为 4.6、5.2、7、14.3 和 11.3 nM。Cabozantinib 显示出抗血管生成活性，破坏肿瘤血管结构，并促进肿瘤和内皮细胞凋亡。

Cabozantinib 化学结构
CAS号：849217-68-1

Cabozantinib 3D分子结构
CAS号：849217-68-1

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Cabozantinib 纯度/质量文件产品仅供科研

货号：A200488 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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c-Kit 亚型比较
FLT3 亚型比较
VEGFR 亚型比较
Tie-2 亚型比较

产品名称	c-Kit ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ c-Kit (Swiss 3T3), IC50: 1.8 μM	PDGFR	99%+
Masitinib	+ Kit, IC50: 200 nM		99%+
Motesanib Diphosphate	+++ Kit, IC50: 8 nM		98%
Ki8751	++ c-Kit, IC50: 40 nM		98+%
Tivozanib	++ c-Kit, IC50: 78 nM		99%+
Pazopanib	+ c-Kit, IC50: 140 nM		99%
Sitravatinib	+++ Kit, IC50: 6 nM		99%+
Pexidartinib	+++ Kit, IC50: 10 nM		99%+
Lactate	++++ c-Kit, IC50: 2 nM	FLT3	85%
Amuvatinib	+++ c-Kit (D816H), IC50: 10 nM		99%+
Imatinib Mesylate	+ c-Kit, IC50: 100 nM	PDGFR	99%
AZD2932	+++ c-Kit, IC50: 9 nM		98%
Axitinib	++++ Kit, IC50: 1.7 nM		98%
Dovitinib	++++ c-Kit, IC50: 2 nM	FLT3	99%+
Sunitinib	✔	FLT3	98%
OSI-930	+ Kit, IC50: 80 nM		99%+
Telatinib	++++ c-Kit, IC50: 1 nM		99%+
Dasatinib monohydrate	++ c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM	Src	98%
Dasatinib	++ c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM	Src	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	FLT3 ↓ ↑	其他靶点	纯度
R406	✔	Syk	98%
Go6976	✔		99%+
Quizartinib	+++ FLT3 (WT), IC50: 4.2 nM FLT3 (ITD), IC50: 1.1 nM		98%
Gilteritinib	++++ FLT3, IC50: 0.29 nM		99%+
Amuvatinib	+ FLT3 (D835Y), IC50: 81 nM		99%+
Pacritinib	++ FLT3 (D835Y), IC50: 6 nM FLT3, IC50: 22 nM		97%
Dovitinib	++++ FLT3, IC50: 1 nM	c-Kit	99%+
Denfivontinib	++++ FLT3 (D835Y), IC50: 0.4 nM FLT3, IC50: 0.4 nM	RET	99%+
TAK-659 HCl	++ FLT3, IC50: 4.6 nM	Syk	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	98%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ VEGFR2, IC50: 25 nM Flk1, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	FGFR,PDGFR,c-Kit	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	c-Kit,BTK	98%
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM	+ hVEGFR3, IC50: 420 nM		98%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			98%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	98+%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	98%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	98%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Tie-2 ↓ ↑	其他靶点	纯度
Tie2 kinase inhibitor 1	++ Tie-2, IC50: 0.25 μM		99%+
MGCD-265 analog	+++ Tie-2, IC50: 7 nM		99%+
Pexmetinib	✔	p38 MAPK	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Cabozantinib 生物活性

靶点

VEGFR2

VEGFR2/KDR, IC50:0.035 nM

描述

The inhibition of VEGF/VEGFR, as well as HGF/c-Met pathway contributes to tumor growth, angiogenesis, invasiveness and metastasis in preclinical studies. Cabozantinib is a potent VEGFR2 inhibitor with IC50 value of 0.035nM, as well as shows inhibitory effect on c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 values of 1.3nM, 4nM, 4.6nM, 12nM/11.3nM/6nM, 14.3nM and 7nM (measured by kinase activity), respectively^[1]. Treatment with Cabozantinib dose-dependently inhibited HGF-induced p-Met at concentration>0.05μM and its downstream p-AKT at concentration>0.1μM in MPNST724 cells, as well as at concentration of 1μM in HUVECs, 0.5μM in ST88 and STS26T cells. The inhibition of VEGFR-2 by Cabozantinib can be observed, as decreased p-VEGFR2, at concentration>0.5μM in HUVECs. Cabozantinib inhibited HGF-induced MPNST cell migration and invasion at 0.5μM for 4h. As prediction by inhibition of Cabozantinib on VEGFR2 and c-Met, Cabozantinib showed potent anti-angiogenesis effect in vivo. The in vivo gel-foam suggested that angiogenesis induced by HGF, VEGF or both decreased (measured based on CD31) by administration of 30mg/kg Cabozantinib for 10 days^[2]. Oral treatment with Cabozantinib for 7 days reduced tumor vascularity by 67% at 3mg/kg and by 83% at 30mg/kg in RIP-Tag2 tumors^[1].

Cabozantinib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
E98NT	0.01-10 μM	Growth Inhibition Assay		IC50=89 nM	23484006
H441		Growth Inhibition Assay		IC50=21700 nM	21926191
H69		Growth Inhibition Assay		IC50=20200 nM	21926191
Hs746T		Growth Inhibition Assay		IC50=9.9 nM	21926191

Cabozantinib 动物研究

Animal Administration

Mice: min = 30 mg/kg^[3], max = 100 mg/kg^[4]

Dose

Mice: 30 mg/kg^[5] (i.p.); 30 mg/kg^[6] (p.o.)

Administration

i.p., p.o.

Pharmacokinetics

Animal	Rats^[7]	Monkeys^[7]
Dose	5 mg/kg	3 mg/kg [formulation: EPW(ethanol:PEG400:water=5:45:50)]
Administration	i.v. or p.o.	i.v. or p.o.
F	111% (p.o.)	73% (p.o.)
AUC_0-inf	259 μM·h (i.v.) 288 μM·h (p.o.)
T_1/2	10.9 h (i.v.) 14.1 h (p.o.)	3.92 h (i.v.) 4.18 h (p.o.)
AUC_0→inf		8.65 μM·h (i.v.) 6.33 μM·h (p.o.)
T_max	0.25 h (i.v.) 4.0 h (p.o.)	0.08 h (i.v.) 3.0 h (p.o.)
CL	0.038 L/kg/h (i.v.)	0.64 L/kg/h (i.v.)
C_max	18.7 μM (i.v.) 14.6 μM (p.o.)	2.51 μM (i.v.) 0.98 μM (p.o.)
Vd_ss	0.6 L/kg (i.v.)	2.67 L/kg (i.v.)
AUC_0→t	196 μM·h (i.v.) 192 μM·h (p.o.)	8.74 μM·h (i.v.) 6.46 μM·h (p.o.)

Cabozantinib 参考文献

[1]You WK, Sennino B, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res. 2011;71(14):4758-68.

[2]Torres KE, Zhu QS, et al. Activated MET is a molecular prognosticator and potential therapeutic target for malignant peripheral nerve sheath tumors. Clin Cancer Res. 2011;17(12):3943-55.

[3]Nguyen HM, Ruppender N, et al. Cabozantinib inhibits growth of androgen-sensitive and castration-resistant prostate cancer and affects bone remodeling. PLoS One. 2013;8(10):e78881.

[4]Navis AC, Bourgonje A, et al. Effects of dual targeting of tumor cells and stroma in human glioblastoma xenografts with a tyrosine kinase inhibitor against c-MET and VEGFR2. PLoS One. 2013;8(3):e58262.

[5]Haider MT, Hunter KD, et al. Rapid modification of the bone microenvironment following short-term treatment with Cabozantinib in vivo. Bone. 2015 Dec;81:581-592.

[6]Yang S, Zhang X, et al. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway. Cancer Gene Ther. 2019 Jun 11.

[7]XL 184

Cabozantinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.97mL

1.99mL

1.00mL

19.94mL

3.99mL

1.99mL

Cabozantinib 技术信息

CAS号	849217-68-1
分子式	C₂₈H₂₄FN₃O₅
分子量	501.506

别名	XL184;BMS-907351
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 25 mg/mL(49.85 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 4.6 mg/mL clear

PO 0.5% CMC-Na 46 mg/mL suspension

卡博替尼 /Cabozantinib {[allProObj[0].p_purity_real_show]}

Cabozantinib 纯度/质量文件产品仅供科研

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卡博替尼 /Cabozantinib {[allProObj[0].p_purity_real_show]}

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