Lenvatinib | E7080;ER-203492-00 | 乐伐替尼 (E7080) | VEGFR

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仑伐替尼 /Lenvatinib {[allProObj[0].p_purity_real_show]}

货号：A336250 同义名： 乐伐替尼 (E7080) / E7080;ER-203492-00

Lenvatinib（E7080）是一种口服、多靶点的酪氨酸激酶抑制剂，靶向VEGFR1-3、FGFR1-4、PDGFR、KIT和RET，显示出强效的抗肿瘤活性。

Lenvatinib 化学结构
CAS号：417716-92-8

Lenvatinib 3D分子结构
CAS号：417716-92-8

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Lenvatinib 纯度/质量文件产品仅供科研

货号：A336250 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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VEGFR 亚型比较

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。

Lenvatinib 生物活性

靶点

VEGFR1

VEGFR1/FLT1, IC50:22 nM
VEGFR3

VEGFR3/FLT4, IC50:5.2 nM
VEGFR2

VEGFR2/KDR, IC50:4.0 nM
FGFR1

FGFR1, IC50:46 nM

描述

SCF is abundantly expressed in a broad spectrum of human malignancies, such asSCLC, NSCLC, colon, breast and renal cancers, acting through both activation of its receptor KIT and paracrine angiogenesis factor. Lenvatinib is a multiple receptor tyrosine kinases inhibitor with IC50 values of 4.0nM, 5.2nM, 22nM, 39nM, 46nM, 51nM and 100nM for VEGFR2, VEGFR3, VEGFR1, PDGFRβ, FGFR1, PDGFRα and Kit (measured by HTRF assays), respectively. Exposure to Lenvatinib inhibited SCF-induced KIT (Tyr719) phosphorylation and VEGF-induced KDR (Tyr996) phosphorylation in HUVEC with IC50 values of 1.9nM and 0.83nM. Consistent with its inhibition of this two targets, the sandwich tube formation (sTF) assay showed that treatment with Lenvatinib inhibited either VEGF or SCF-induced tube formation of HUVEC in a dose-dependent manner with IC50s of 5.2 and 5.1nM, respectively. Though Lenvatinib did not show the potent inhibitory activities against H146 cells expressing SCF, but not KIT, it inhibited SCF-induced cell proliferation of human SCLC, H526 cells expressing KIT, suggesting the inhibition by Lenvatinib on cell growth through paracrine. Oral administration of Lenvatinib at dose of 30 and 100 mg/kg (BID, QDx21) caused tumor growth in a dose-dependent manner in H146 xenograft, while tumor regression achieved at dose of 100mg/kg with decreased microvessel density^[1].

Lenvatinib 动物研究

Dose

Mice: 3 mg/kg - 100 mg/kg^[1] (p.o.)

Administration

p.o.

Pharmacokinetics

Animal	Mice^[2]	Rats^[2]	Dogs^[2]	Monkeys^[2]
Dose	3 mg/kg	3 mg/kg	3 mg/kg	3 mg/kg
Administration	i.v. or p.o.	i.v. or p.o.	i.v. or p.o.	i.v. or p.o.
F	64.4% (p.o.)	68.7% (p.o.)	70.4% (p.o.)	78.4% (p.o.)
AUC_0→inf	8.686 μg·h/ml (i.v.) 5.596 μg·h/ml (p.o.)		8.417 μg·h/ml (i.v.) 5.481 μg·h/ml (p.o.)	12.900 μg·h/ml (i.v.) 10.272 μg·h/ml (p.o.)
T_1/2	2.05 h (i.v.) 2.09 h (p.o.)	3.65 h (i.v.) 3.61 h (p.o.)	5.27 h (i.v.) 4.76 h (p.o.)	4.28 h (i.v.) 4.07 h (p.o.)
T_max	0.5 h (p.o.)	0.5 h (p.o.)	2 h (p.o.)	2 h (p.o.)
CL_p	345.4 ml/h/kg (i.v.)	100.2 ml/h/kg (i.v.)	368.3 ml/h/kg (i.v.)	237.7 ml/h/kg (i.v.)
AUC_0-inf		30.107 μg·h/ml (i.v.) 20.697 μg·h/ml (p.o.)
C_max	7.0542 μg/ml (i.v.) 1.9651 μg/ml (p.o.)	14.0567 μg/ml (i.v.) 6.1671 μg/ml (p.o.)	2.2889 μg/ml (i.v.) 1.2717 μg/ml (p.o.)	4.6427 μg/ml (i.v.) 2.5013 μg/ml (p.o.)
Vss	714.3 ml/kg (i.v.)	391.5 ml/kg (i.v.)	1610.0 ml/kg (i.v.)	793.7 ml/kg (i.v.)

Lenvatinib 参考文献

[1]Tohyama O, Matsui J, et al. Antitumor activity of lenvatinib (e7080): an angiogenesis inhibitor that targets multiple receptor tyrosine kinases in preclinical human thyroid cancer models. J Thyroid Res. 2014;2014:638747.

[2]Lenvatinib

Lenvatinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.71mL

2.34mL

1.17mL

23.43mL

4.69mL

2.34mL

Lenvatinib 技术信息

CAS号	417716-92-8
分子式	C₂₁H₁₉ClN₄O₄
分子量	426.85

别名	乐伐替尼 (E7080) ;E7080;ER-203492-00
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 12 mg/mL(28.11 mM)，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

0.5% methylcellulose+water 30 mg/mL suspension

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Lenvatinib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Lenvatinib 质控信息

Lenvatinib 生物活性

Lenvatinib 动物研究

Lenvatinib 参考文献

Lenvatinib 实验方案

Lenvatinib 技术信息

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VEGFR1	VEGFR1/FLT1, IC50:22 nM
VEGFR3	VEGFR3/FLT4, IC50:5.2 nM
VEGFR2	VEGFR2/KDR, IC50:4.0 nM
FGFR1	FGFR1, IC50:46 nM

仑伐替尼 /Lenvatinib {[allProObj[0].p_purity_real_show]}

Lenvatinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Lenvatinib 质控信息

Lenvatinib 生物活性

Lenvatinib 动物研究

Lenvatinib 参考文献

Lenvatinib 实验方案

Lenvatinib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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C

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Lenvatinib 纯度/质量文件产品仅供科研