Cabozantinib S-malate | XL184 S-malate;BMS-907351 S-malate;XL184;Cabozantinib malate | 苹果酸卡博替尼 (XL184) | VEGFR | TAM Receptor

Cabozantinib S-malate/卡博替尼苹果酸盐 {[allProObj[0].p_purity_real_show]}

货号：A212266 同义名： 苹果酸卡博替尼 (XL184) / XL184 S-malate; BMS-907351 S-malate

Cabozantinib S-malate (XL184 S-malate) 是一种多受体酪氨酸激酶的强效抑制剂，包括 VEGFR2、c-Met、Kit、Axl 和 Flt3，IC50 值分别为 0.035、1.3、4.6、7 和 11.3 nM。

Cabozantinib S-malate/卡博替尼苹果酸盐化学结构
CAS号：1140909-48-3

Cabozantinib S-malate/卡博替尼苹果酸盐 3D分子结构
CAS号：1140909-48-3

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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/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	RET,PDGFR	97%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ Flk1, IC50: 25 nM VEGFR2, 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	c-Kit,PDGFR,FGFR	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	c-Kit,FLT3	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/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms/CSF1R	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	BTK,c-Kit	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	+++ hVEGFR2, IC50: 9 nM mVEGF2, IC50: 165 nM	+ hVEGFR3, IC50: 420 nM		99%
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			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Apatinib 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	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2/Flk1, IC50: 90 nM VEGFR2, 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	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	RET,FLT3	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。

Cabozantinib S-malate/卡博替尼苹果酸盐生物活性

靶点

VEGFR2

VEGFR2/KDR, IC50:0.035 nM

描述

Cabozantinib S-malate is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.

Cabozantinib S-malate/卡博替尼苹果酸盐细胞实验

Cell Line HLE MHCC97-H ACHN 786-0 HepG2NTCP cells RAW264.7 pre-osteoclasts MC3T3-E1 pre-osteoblasts	Concentration	Treated Time	Description	References
HLE	IC50	24 h	Inhibited cell cycle progression, reduced proliferation, and induced apoptosis	Gut. 2021 Sep;70(9):1746-1757.
MHCC97-H	IC50	24 h	Inhibited cell cycle progression, reduced proliferation, and induced apoptosis	Gut. 2021 Sep;70(9):1746-1757.
ACHN	1–30 μM	24 h	To evaluate the effect of Cabozantinib on the viability of renal cancer cells, showing a dose-dependent decrease in cell viability.	Redox Biol. 2023 Dec;68:102945.
786-0	1–30 μM	24 h	To evaluate the effect of Cabozantinib on the viability of renal cancer cells, showing a dose-dependent decrease in cell viability.	Redox Biol. 2023 Dec;68:102945.
HepG2NTCP cells	100 nM	7 days	Cabozantinib inhibits HBV RNA transcription by decreasing the binding of phosphorylated STAT3 to the enhancer region 1 of cccDNA through the HGF-MET-STAT3 signaling axis.	Hepatol Commun. 2023 Nov 8;7(11):e0313.
RAW264.7 pre-osteoclasts	100 nM and 500 nM	5 days	Cabozantinib inhibited RANKL-induced differentiation of RAW264.7 cells into osteoclasts, reducing TRAP activity by 26% and 50%, respectively.	Mol Cancer Ther. 2020 Jun;19(6):1266-1278.
MC3T3-E1 pre-osteoblasts	100 nM	6 days	Cabozantinib enhanced osteoblast differentiation, as demonstrated by increases in mRNA and protein levels of ALP and OSC, as well as in calcium deposits.	Mol Cancer Ther. 2020 Jun;19(6):1266-1278.

Cell Line

HLE MHCC97-H ACHN 786-0 HepG2NTCP cells RAW264.7 pre-osteoclasts MC3T3-E1 pre-osteoblasts

Concentration

Treated Time

Description

References

HLE

IC50

24 h

Inhibited cell cycle progression, reduced proliferation, and induced apoptosis

Gut. 2021 Sep;70(9):1746-1757.

MHCC97-H

IC50

24 h

Inhibited cell cycle progression, reduced proliferation, and induced apoptosis

Gut. 2021 Sep;70(9):1746-1757.

ACHN

1–30 μM

24 h

To evaluate the effect of Cabozantinib on the viability of renal cancer cells, showing a dose-dependent decrease in cell viability.

Redox Biol. 2023 Dec;68:102945.

786-0

1–30 μM

24 h

To evaluate the effect of Cabozantinib on the viability of renal cancer cells, showing a dose-dependent decrease in cell viability.

Redox Biol. 2023 Dec;68:102945.

HepG2NTCP cells

100 nM

7 days

Cabozantinib inhibits HBV RNA transcription by decreasing the binding of phosphorylated STAT3 to the enhancer region 1 of cccDNA through the HGF-MET-STAT3 signaling axis.

Hepatol Commun. 2023 Nov 8;7(11):e0313.

RAW264.7 pre-osteoclasts

100 nM and 500 nM

5 days

Cabozantinib inhibited RANKL-induced differentiation of RAW264.7 cells into osteoclasts, reducing TRAP activity by 26% and 50%, respectively.

Mol Cancer Ther. 2020 Jun;19(6):1266-1278.

MC3T3-E1 pre-osteoblasts

100 nM

6 days

Cabozantinib enhanced osteoblast differentiation, as demonstrated by increases in mRNA and protein levels of ALP and OSC, as well as in calcium deposits.

Mol Cancer Ther. 2020 Jun;19(6):1266-1278.

Cabozantinib S-malate/卡博替尼苹果酸盐动物实验

Species Mice Nude mice Mice SCID mice C57BL/6J mice	Animal Model C-Met/β-catenin, Akt/c-Met, Akt/Ras, c-Myc HCC models Renal cancer xenograft model Liver cancer model Bo-786 RCC bone metastasis model HCC mouse model	Administration	Dosage	Frequency	Description	References
Mice	C-Met/β-catenin, Akt/c-Met, Akt/Ras, c-Myc HCC models	Oral	60 mg/kg	Once daily for 3 weeks	In c-Met/β-catenin and Akt/c-Met models, Cabozantinib treatment led to stable disease, but it was ineffective in Akt/Ras and c-Myc models	Gut. 2021 Sep;70(9):1746-1757.
Nude mice	Renal cancer xenograft model	Intraperitoneal injection	15 mg/kg	Every alternate day for three weeks	To evaluate the effect of Cabozantinib and Honokiol combination therapy on tumor growth in a renal cancer xenograft model, showing significant inhibition of tumor growth.	Redox Biol. 2023 Dec;68:102945.
Mice	Liver cancer model	Oral	30 mg/kg	Daily until the end of the study	Cabozantinib alone significantly increased neutrophil infiltration and reduced intra-tumour CD8+PD1+T cell proportions, while the combination with anti-PD1 further stimulated both effects and significantly decreased Treg infiltration.	Clin Cancer Res. 2022 Jun 1;28(11):2449-2460
SCID mice	Bo-786 RCC bone metastasis model	Oral gavage	20 mg/kg	Twice daily, 6 days a week for 18 to 39 days	Cabozantinib inhibited the growth of Bo-786 RCC in bone, reduced bone osteolysis, increased bone volume and osteoblast number, and decreased osteoclast number and blood vessel density.	Mol Cancer Ther. 2020 Jun;19(6):1266-1278.
C57BL/6J mice	HCC mouse model	Oral	30 mg/kg	Daily until the end of the study	The combination of cabozantinib and anti-PD1 showed increased anti-tumour efficacy compared to monotherapy and placebo, significantly increasing neutrophil infiltration and reducing intra-tumour CD8+PD1+T cell proportions, while significantly decreasing Treg infiltration.	Clin Cancer Res. 2022 Jun 1;28(11):2449-2460

Species

Mice Nude mice Mice SCID mice C57BL/6J mice

Animal Model

C-Met/β-catenin, Akt/c-Met, Akt/Ras, c-Myc HCC models Renal cancer xenograft model Liver cancer model Bo-786 RCC bone metastasis model HCC mouse model

Administration

Dosage

Frequency

Description

References

Mice

C-Met/β-catenin, Akt/c-Met, Akt/Ras, c-Myc HCC models

Oral

60 mg/kg

Once daily for 3 weeks

In c-Met/β-catenin and Akt/c-Met models, Cabozantinib treatment led to stable disease, but it was ineffective in Akt/Ras and c-Myc models

Gut. 2021 Sep;70(9):1746-1757.

Nude mice

Renal cancer xenograft model

Intraperitoneal injection

15 mg/kg

Every alternate day for three weeks

To evaluate the effect of Cabozantinib and Honokiol combination therapy on tumor growth in a renal cancer xenograft model, showing significant inhibition of tumor growth.

Redox Biol. 2023 Dec;68:102945.

Mice

Liver cancer model

Oral

30 mg/kg

Daily until the end of the study

Cabozantinib alone significantly increased neutrophil infiltration and reduced intra-tumour CD8+PD1+T cell proportions, while the combination with anti-PD1 further stimulated both effects and significantly decreased Treg infiltration.

Clin Cancer Res. 2022 Jun 1;28(11):2449-2460

SCID mice

Bo-786 RCC bone metastasis model

Oral gavage

20 mg/kg

Twice daily, 6 days a week for 18 to 39 days

Cabozantinib inhibited the growth of Bo-786 RCC in bone, reduced bone osteolysis, increased bone volume and osteoblast number, and decreased osteoclast number and blood vessel density.

Mol Cancer Ther. 2020 Jun;19(6):1266-1278.

C57BL/6J mice

HCC mouse model

Oral

30 mg/kg

Daily until the end of the study

The combination of cabozantinib and anti-PD1 showed increased anti-tumour efficacy compared to monotherapy and placebo, significantly increasing neutrophil infiltration and reducing intra-tumour CD8+PD1+T cell proportions, while significantly decreasing Treg infiltration.

Clin Cancer Res. 2022 Jun 1;28(11):2449-2460

Cabozantinib S-malate/卡博替尼苹果酸盐参考文献

Cabozantinib S-malate/卡博替尼苹果酸盐实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.87mL

1.57mL

0.79mL

15.73mL

3.15mL

1.57mL

Cabozantinib S-malate/卡博替尼苹果酸盐技术信息

CAS号	1140909-48-3
分子式	C₃₂H₃₀FN₃O₁₀
分子量	635.59
SMILES Code	O=C(O)[C@@H](O)CC(O)=O.O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=CC=NC5=CC(OC)=C(OC)C=C45)C=C3
MDL No.	MFCD20923480

别名	苹果酸卡博替尼 (XL184) ;XL184 S-malate; BMS-907351 S-malate; XL184; Cabozantinib malate
运输	蓝冰
InChI Key	HFCFMRYTXDINDK-WNQIDUERSA-N
Pubchem ID	25102846

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(165.2 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

Cabozantinib S-malate/卡博替尼苹果酸盐 {[allProObj[0].p_purity_real_show]}

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Cabozantinib S-malate/卡博替尼苹果酸盐细胞实验

Cabozantinib S-malate/卡博替尼苹果酸盐动物实验

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