Cabozantinib (Synonyms: 卡博替尼; XL184; BMS-907351)

目錄號: HY-13016 純度: 99.96%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Cabozantinib 是一種口服有效的 VEGFR2 和 MET 抑制劑，IC₅₀ 分別為 0.035 和 1.3 nM。Cabozantinib 對 KIT、RET、AXL、TIE2 和 FLT3 有較強的抑制作用 (IC₅₀=4.6、5.2、7、14.3 和 11.3 nM)。Cabozantinib 顯示出抗血管生成活性。Cabozantinib 可以破壞腫瘤血管，促進腫瘤和內(nèi)皮細胞凋亡 (apoptosis)。

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Cabozantinib Chemical Structure

CAS No. : 849217-68-1

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規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥861	In-stock
1 mg	￥345	In-stock
5 mg	￥780	In-stock
10 mg	￥1100	In-stock
25 mg	￥1938	In-stock
50 mg	￥2850	In-stock
100 mg	￥4000	In-stock
200 mg	￥5450	In-stock
500 mg	現(xiàn)貨	詢價
1 g		詢價
5 g		詢價

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Other Forms of Cabozantinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 43 篇科研文獻

•Cancer Discov. 2021 Jan;11(1):126-141. [Abstract]
•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
•Biomaterials. 16 September 2022.
•Br J Cancer. 2024 Jun 20. [Abstract]
•Adv Healthc Mater. 2023 Aug 21;e2302046. [Abstract]
•Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]

•Cancer Lett. 2019 Apr 10;447:105-114. [Abstract]
•J Transl Med. 2023 Jan 9;21(1):9. [Abstract]
•J Pharm Anal. 2021 Jun 19.
•J Med Chem. 2016 Jan 14;59(1):358-73. [Abstract]
•BMC Biol. 2024 Oct 1;22(1):222. [Abstract]
•Cancers (Basel). 2024 Jan 8, 16(2), 269.
•Invest Ophthalmol Vis Sci. 2022 Dec 1;63(13):14. [Abstract]
•Int J Mol Sci. 2022 Sep 14;23(18):10677.
•Front Oncol. 2022 Jul 7;12:915319. [Abstract]
•Antioxidants (Basel). 2021, 10(9), 1336.
•Biomedicines. 2020 Nov 28;8(12):547. [Abstract]
•J Neurosci. 2020 Dec 9;40(50):9602-9616. [Abstract]
•Sci Rep. 2019 Nov 12;9(1):16600. [Abstract]
•Mol Cancer Res. 2019 Feb;17(2):499-507. [Abstract]
•Drug Des Devel Ther. 2018 Apr 30;12:1009-1017. [Abstract]
•Mol Cancer Ther. 2017 Nov;16(11):2387-2398. [Abstract]
•Spectrochim Acta A Mol Biomol Spectrosc. 2016 Apr 15;159:199-208. [Abstract]
•Biochem Biophys Res Commun. 2024 Nov 19:734:150781. [Abstract]
•Saudi Pharm J. 2023 Aug 24, 101756.
•Virology. 2023 Jun 21.
•Fundam Clin Pharmacol. 2021 Feb 1. [Abstract]
•Am J Reprod Immunol. 2021 Mar;85(3):e13352. [Abstract]
•Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
•J Cell Biochem. 2020 Mar;121(3):2343-2353. [Abstract]
•PLoS One. 2017 Sep 25;12(9):e0185321. [Abstract]
•Biomed Chromatogr. 2024 Jan 30:e5833. [Abstract]
•Biomed Chromatogr. 2023 May 15;e5685. [Abstract]
•React Kinet Mech Cat. 07 January 2022.
•Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11. [Abstract]
•Biomed Chromatogr. 2020 Aug;34(8):e4862. [Abstract]
•bioRxiv. 2024 November 03.
•bioRxiv. 2023 Apr 14.
•Patent. US20220332731A1.
•Mediat Inflamm. 2020 Oct 24;2020:1649453. [Abstract]
•Biochem Biophys Rep. 2020 Jan 17;21:100726. [Abstract]
•Patent. US20170349880A1.
•Harvard Medical School LINCS LIBRARY

: Cabozantinib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Nov;16(11):2387-2398. [Abstract]; Representative Western blots and densitometry show that cabozantinib reduces phosphorylation of Erk1/2 after 6 hours and reduces cyclin D1 and increases p27 protein levels after 24 hours of treatment (n=3-4).

: Cabozantinib purchased from MCE. Usage Cited in: PLoS One. 2017 Sep 25;12(9):e0185321. [Abstract]; Treatment with Cabozantinib results in complete inhibition of the c-MET phosphorylation stimulated by HGF at nanomolar concentrations.

: Cabozantinib purchased from MCE. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73. [Abstract]; Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R

: Cabozantinib purchased from MCE. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73. [Abstract]; Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R

Cabozantinib 相關(guān)產(chǎn)品

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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Axl Mer Tyro3

生物活性
純度 & 產(chǎn)品資料
參考文獻

生物活性

Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC₅₀ values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC₅₀=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis^[1]^[2].

IC₅₀ & Target^[1]

VEGFR2

0.035 nM (IC₅₀)

Axl

Flt-4

6 nM (IC₅₀)

Flt-1

12 nM (IC₅₀)

Met

1.3 ± 1.2 nM (IC₅₀)

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A498	IC₅₀	8456 nM Compound: Cabozantinib	Antiproliferative activity against human A498 cells after 48 hrs by MTT assay Antiproliferative activity against human A498 cells after 48 hrs by MTT assay	[PMID: 29057042]
A549	IC₅₀	≥ 50 nM Compound: Cabozantinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30248654]
A549	IC₅₀	0.33 μM Compound: XL-184	Antiproliferative activity against human A549 cells expressing c-Met after 48 hrs by MTT assay Antiproliferative activity against human A549 cells expressing c-Met after 48 hrs by MTT assay	[PMID: 35227978]
A549	IC₅₀	0.76 μM Compound: 1; XL-184	Cytotoxicity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 33601310]
A549	IC₅₀	15.23 μM Compound: Cabozantinib	Antiproliferation activity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Antiproliferation activity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 34186178]
A549	IC₅₀	3.75 μM Compound: Cabozantinib	Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
A549	IC₅₀	4205 nM Compound: Cabozantinib	Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
A549	IC₅₀	7.21 μM Compound: Cabozantinib	Antiproliferative against human A549 cells assessed as reduction in cell viability by MTT assay Antiproliferative against human A549 cells assessed as reduction in cell viability by MTT assay	[PMID: 33045329]
A549	IC₅₀	7.8 μM Compound: XL-184	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32738414]
A549	IC₅₀	8.5 μM Compound: Cabozantinib	Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay	[PMID: 30940564]
A549	IC₅₀	9.52 μM Compound: Cabozantinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30503936]
A549/CDDP	IC₅₀	19.6 μM Compound: Cabozantinib	Antiproliferative activity against human A549/CDDP cells after 72 hrs by MTT assay Antiproliferative activity against human A549/CDDP cells after 72 hrs by MTT assay	[PMID: 30503936]
BaF3	GI₅₀	> 10 μM Compound: Cabozantinib	Cytotoxicity against mouse BA/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay Cytotoxicity against mouse BA/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay	[PMID: 27814560]
BaF3	GI₅₀	0.01 μM Compound: Cabozantinib	Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	IC₅₀	0.0219 μM Compound: Cabozantinib	Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay	[PMID: 27068889]
BaF3	IC₅₀	0.024 μM Compound: Cabozantinib	Antiproliferative activity against mouse BAF3 cells harboring TRP-MET after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BAF3 cells harboring TRP-MET after 72 hrs by CCK-8 assay	[PMID: 29146452]
BaF3	GI₅₀	0.05 μM Compound: Cabozantinib	Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	0.15 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells over expressing wild type RET incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells over expressing wild type RET incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	IC₅₀	0.18 μM Compound: 2	Inhibition of RET V804M mutant (unknown origin)expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay Inhibition of RET V804M mutant (unknown origin)expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay	[PMID: 32292556]
BaF3	GI₅₀	0.89 μM Compound: Cabozantinib	Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	0.91 μM Compound: Cabozantinib	Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	1.45 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells harboring RET M918T mutant incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells harboring RET M918T mutant incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	GI₅₀	1.53 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells harboring RET V804L mutant incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells harboring RET V804L mutant incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	IC₅₀	14 nM Compound: 2	Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay	[PMID: 26874741]
BaF3	IC₅₀	190 nM Compound: 2	Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay	[PMID: 26874741]
BaF3	GI₅₀	2.8 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells harboring RET V804M mutant incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells harboring RET V804M mutant incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	IC₅₀	7.5 μM Compound: XL184; BMS-907351	Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrs Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrs	[PMID: 26717201]
BaF3	GI₅₀	7.914 μM Compound: Cabozantinib	Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay	[PMID: 32882611]
BaF3	IC₅₀	889 nM Compound: Cabozantinib	Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
BaF3	GI₅₀	9.36 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells incubated for 3 days by MTT assay	[PMID: 29133048]
CAKI-1	IC₅₀	1.66 μM Compound: Cabozantinib	Cytotoxicity against human CAKI-1 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human CAKI-1 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
EBC-1	IC₅₀	4.8 nM Compound: Cabozantinib	Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay	[PMID: 30248654]
EBC-1	IC₅₀	51.4 nM Compound: Cabozantinib	Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay	[PMID: 28412159]
FHC	IC₅₀	4.4 μM Compound: Cabozantinib	Cytotoxicity against human FHC cells after 72 hrs by MTT assay Cytotoxicity against human FHC cells after 72 hrs by MTT assay	[PMID: 30503936]
HCT-116	IC₅₀	3.78 μM Compound: Cabozantinib	Cytotoxicity against human HCT-116 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
HCT-116	IC₅₀	4.67 μM Compound: XL-184	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32738414]
HEK293	IC₅₀	25.8 μM Compound: JV-985	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 33214822]
HeLa	IC₅₀	> 10000 nM Compound: XL184	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
HeLa	IC₅₀	> 20 μM Compound: Cabozantinib	Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31307762]
HeLa	IC₅₀	0.32 μM Compound: 1; XL-184	Cytotoxicity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 33601310]
HeLa	IC₅₀	79.06 μM Compound: XL-184	Antiproliferative activity against human HeLa cells expressing c-Met after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells expressing c-Met after 48 hrs by MTT assay	[PMID: 35227978]
HepG2	IC₅₀	12 nM Compound: Cabozantinib	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 28412159]
HepG2	IC₅₀	15.58 μM Compound: Cabozantinib	Antiproliferation activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Antiproliferation activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 34186178]
HepG2	IC₅₀	3.05 μM Compound: Cabozantinib	Cytotoxicity against human HepG2 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
HepG2	IC₅₀	8.3 μM Compound: JV-985	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 33214822]
HL-60	IC₅₀	22.46 μM Compound: Cabozantinib	Antiproliferative activity against human HL60 cells harboring wild type FLT3 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells harboring wild type FLT3 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 31466809]
HT-29	IC₅₀	10.6 μM Compound: Cabozantinib	Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 32731184]
HT-29	IC₅₀	11.5 μM Compound: Cabozantinib	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 30503936]
HT-29	IC₅₀	4.56 μM Compound: Cabozantinib	Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
HT-29	IC₅₀	53 μM Compound: Cpd I	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32113049]
HT-29	IC₅₀	9.6 μM Compound: Cabozantinib	Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31307762]
HT-29	IC₅₀	9.6 μM Compound: Cabozantinib	Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay	[PMID: 30940564]
Huh-7	IC₅₀	4348 nM Compound: Cabozantinib	Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay	[PMID: 29057042]
HUVEC	IC₅₀	45 nM Compound: Cabozantinib	Cytotoxicity against HUVEC after 96 hrs by MTT assay Cytotoxicity against HUVEC after 96 hrs by MTT assay	[PMID: 30248654]
HUVEC	IC₅₀	7.8 μM Compound: XL184; BMS-907351	Inhibition of VEGFR-2 phosphorylation in HUVEC incubated for 1 to 3 hrs Inhibition of VEGFR-2 phosphorylation in HUVEC incubated for 1 to 3 hrs	[PMID: 26717201]
HUVEC	IC₅₀	7670 nM Compound: XL184	Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
L02	IC₅₀	54.97 μM Compound: 1; XL-184	Cytotoxicity against human L02 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 33601310]
MCF7	IC₅₀	0.45 μM Compound: 1; XL-184	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 33601310]
MCF7	IC₅₀	14.26 μM Compound: Cabozantinib	Antiproliferation activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Antiproliferation activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 34186178]
MCF7	IC₅₀	2889 nM Compound: Cabozantinib	Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
MCF7	IC₅₀	30.87 μM Compound: XL-184	Antiproliferative activity against human MCF7 cells expressing c-Met after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells expressing c-Met after 48 hrs by MTT assay	[PMID: 35227978]
MCF7	IC₅₀	5.4 μM Compound: Cabozantinib	Antiproliferative against human MCF-7 cells assessed as reduction in cell viability by MTT assay Antiproliferative against human MCF-7 cells assessed as reduction in cell viability by MTT assay	[PMID: 33045329]
MCF7	IC₅₀	5.98 μM Compound: XL-184	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32738414]
MCF7	IC₅₀	8.57 μM Compound: Cabozantinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30503936]
MDA-MB-231	IC₅₀	13.4 μM Compound: Cabozantinib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 30503936]
MDA-MB-231	IC₅₀	19.72 μM Compound: Cabozantinib	Antiproliferation activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Antiproliferation activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 34186178]
MDA-MB-231	IC₅₀	42 μM Compound: XL184; BMS-907351	Inhibition of KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrs Inhibition of KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrs	[PMID: 26717201]
MDA-MB-231	IC₅₀	5 μM Compound: XL184; BMS-907351	Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrs Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrs	[PMID: 26717201]
MDA-MB-231	IC₅₀	5080 nM Compound: XL184	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
MKN-45	IC₅₀	32 μM Compound: Cpd I	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32113049]
MKN-45	IC₅₀	6.9 nM Compound: Cabozantinib	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 30248654]
MV4-11	IC₅₀	15.16 μM Compound: Cabozantinib	Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 31466809]
NCI-H1299	IC₅₀	1919 nM Compound: Cabozantinib	Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
NCI-H1975	IC₅₀	6.67 μM Compound: Cabozantinib	Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31307762]
NCI-H292	IC₅₀	≥ 50 nM Compound: Cabozantinib	Antiproliferative activity against human NCI-H292 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H292 cells after 72 hrs by MTT assay	[PMID: 30248654]
NCI-H460	IC₅₀	3.6 μM Compound: Cpd I	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32113049]
NCI-H460	IC₅₀	40.1 nM Compound: Cabozantinib	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 30248654]
NCI-H460	IC₅₀	5669 nM Compound: Cabozantinib	Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
NCI-H727	IC₅₀	14010 nM Compound: Cabozantinib	Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay	[PMID: 29057042]
NIH3T3	GI₅₀	> 10 μM Compound: Cabozantinib	Growth inhibition of human NIH3T3 cells incubated for 3 days by MTT assay Growth inhibition of human NIH3T3 cells incubated for 3 days by MTT assay	[PMID: 29133048]
NIH3T3	GI₅₀	0.1 μM Compound: Cabozantinib	Growth inhibition of human NIH3T3 cells harboring RET C634Y mutant incubated for 3 days by MTT assay Growth inhibition of human NIH3T3 cells harboring RET C634Y mutant incubated for 3 days by MTT assay	[PMID: 29133048]
PANC-1	IC₅₀	5.13 μM Compound: Cabozantinib	Cytotoxicity against human PANC-1 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human PANC-1 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
PC-3	IC₅₀	1.9 μM Compound: XL184; BMS-907351	Inhibition of c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrs Inhibition of c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrs	[PMID: 26717201]
PC-3	IC₅₀	3.68 μM Compound: Cabozantinib	Cytotoxicity against human PC-3 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human PC-3 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
PC-3	IC₅₀	8.25 μM Compound: Cabozantinib	Antiproliferative activity against human PC-3 cells measured after 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
Sf21	IC₅₀	16 nM Compound: 2	Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay	[PMID: 26874741]
Sf21	IC₅₀	3 nM Compound: Cabozantinib	Inhibition of wild type N-terminal GST-tagged recombinant human RET (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA Inhibition of wild type N-terminal GST-tagged recombinant human RET (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA	[PMID: 27131066]
Sf21	IC₅₀	811 nM Compound: Cabozantinib	Inhibition of N-terminal GST-tagged recombinant human RET V804M mutant (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA Inhibition of N-terminal GST-tagged recombinant human RET V804M mutant (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA	[PMID: 27131066]
SiHa	IC₅₀	7940 nM Compound: XL184	Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
SNU-5	IC₅₀	12.1 nM Compound: Cabozantinib	Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay	[PMID: 30248654]
SW-620	IC₅₀	3.37 μM Compound: Cabozantinib	Cytotoxicity in human SW620 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human SW620 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31307762]
T47D	IC₅₀	4448 nM Compound: Cabozantinib	Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
T47D	IC₅₀	4790 nM Compound: XL184	Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
TT	GI₅₀	0.12 μM Compound: Cabozantinib	Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay	[PMID: 26652860]

體外研究
(In Vitro)

Cabozantinib 抑制 MET 和 VEGFR2 以及 KIT、FLT3 和 AXL 的磷酸化，IC₅₀ 值分別為 7.8、1.9、5.0、7.5 和 42 μM^[1]。
Cabozantinib (4.6 nM) 抑制小管形成，且無細胞毒性證據(jù)，在 HMVEC、MDA-MB-231、A431、HT1080 和 B16F10 細胞中的 IC₅₀ 值分別為 6.7、5.1、4.1、7.7 和 4.7 nM^[1]。
Cabozantinib (0-370 nM, 24 h) 抑制細胞遷移和侵襲^[1]。
Cabozantinib (48 h) 能抑制多種腫瘤細胞的增殖^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells^[1]
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^[1]
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^[1]
Concentration:	0, 1.5, 14, and 123 nM
Incubation Time:	24 hours
Result:	Potently inhibited HGF-induced invasion (IC₅₀ = 9 nM) of B16F10 cells.

體內(nèi)研究
(In Vivo)

Cabozantinib (100 mg/kg; p.o.，單劑量) 可抑制小鼠的 MET 和 VEGFR2 磷酸化^[1]。
Cabozantinib (100 mg/kg; p.o.，單劑量) 顯著增加腫瘤缺氧和細胞凋亡^[1]。
Cabozantinib（0-60 mg/kg; p.o.，每天一次，連續(xù) 14 天）以劑量依賴性方式抑制腫瘤生長^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female mice bearing MBA-MB-231 tumor (5 per group)^[1]
Dosage:	0, 100 mg/kg
Administration:	Orally, once
Result:	Inhibited MET and VEGFR2 phosphorylation.

Animal Model:	Mice bearing MBA-MB-231 tumor^[1]
Dosage:	1, 3, 10, 30, 60 mg/kg
Administration:	Orally, once daily for 14 days
Result:	Inhibited tumor growth in a dose-dependent manner.

Clinical Trial

分子量

501.51

Formula

C₂₈H₂₄FN₃O₅

CAS 號

849217-68-1

性狀

固體

顏色

White to gray

中文名稱

卡博替尼

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : 25 mg/mL (49.85 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.9940 mL	9.9699 mL	19.9398 mL
5 mM	0.3988 mL	1.9940 mL	3.9880 mL
10 mM	0.1994 mL	0.9970 mL	1.9940 mL

查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year (protect from light)。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

摩爾計算器
稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.98 mM); 澄清溶液
方案二

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.15 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案三

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.15 mM); 懸濁液; 超聲助溶

此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案四

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.15 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

方案一

請依序添加每種溶劑： 0.5% CMC/saline water
Solubility: 2.5 mg/mL (4.98 mM); 懸濁液; 超聲助溶

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購。，Tween 80，均可在 MCE 網(wǎng)站選購。

計算結(jié)果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。

動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.96%

選擇批次：

Data Sheet (647 KB) SDS (393 KB)

COA (196 KB) LCMS (110 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻

[1]. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308. [Content Brief]

[2]. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768. [Content Brief]

[3]. Fuse MA, et al. Combination Therapy With c-Met and Src Inhibitors Induces Caspase-Dependent Apoptosis of Merlin-Deficient Schwann Cells and Suppresses Growth of Schwannoma Cells. Mol Cancer Ther. Mol Cancer Ther. 2017 Nov;16(11):2387-2398. [Content Brief]

Cabozantinib 相關(guān)分類

Cancer

完整儲備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9940 mL	9.9699 mL	19.9398 mL	49.8495 mL
	5 mM	0.3988 mL	1.9940 mL	3.9880 mL	9.9699 mL
	10 mM	0.1994 mL	0.9970 mL	1.9940 mL	4.9849 mL
	15 mM	0.1329 mL	0.6647 mL	1.3293 mL	3.3233 mL
	20 mM	0.0997 mL	0.4985 mL	0.9970 mL	2.4925 mL
	25 mM	0.0798 mL	0.3988 mL	0.7976 mL	1.9940 mL
	30 mM	0.0665 mL	0.3323 mL	0.6647 mL	1.6616 mL
	40 mM	0.0498 mL	0.2492 mL	0.4985 mL	1.2462 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MCE 顧客使用本產(chǎn)品發(fā)表的 43 篇科研文獻

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生物活性

純度 & 產(chǎn)品資料

參考文獻

摩爾計算器

稀釋計算器

Cabozantinib 相關(guān)分類

完整儲備液配制表

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Cabozantinib (Synonyms: 卡博替尼; XL184; BMS-907351)

Customer Review

Other Forms of Cabozantinib:

Cabozantinib 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 43 篇科研文獻

Cabozantinib 相關(guān)產(chǎn)品

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查看 VEGFR 亞型特異性產(chǎn)品:

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生物活性

純度 & 產(chǎn)品資料

參考文獻

Cabozantinib 相關(guān)抗體:

摩爾計算器

稀釋計算器

Cabozantinib 相關(guān)分類

完整儲備液配制表

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