Fruquintinib (Synonyms: HMPL-013)

Name: Fruquintinib
Brand: MedChemExpress
SKU: HY-19912
Rating: 5.0 (10 reviews)

Cat. No.: HY-19912 Purity: 99.98%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC₅₀s of 33, 0.35, and 35 nM, respectively.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 1194506-26-7

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 10 publication(s) in Google Scholar

Other Forms of Fruquintinib:

Fruquintinib-d₆ In-stock
Fruquintinib (Standard) 견적 받기

10 Publications Citing Use of MCE Fruquintinib

Histological Imaging/Staining

In Vivo Efficacy Study

Cell Imaging/Staining

: Fruquintinib purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Dec;31(12):1625-1635. [Abstract]; The angiogenesis inhibitor Fruquintinib (Fq) (2 mg/kg; i.g.; once daily) effectively inhibited the expression of CD31 and enhanced the inhibition of 2,5-AM on CD31 in HPAC and MIA Paca2 cell xenograft tumor tissues.

: Fruquintinib purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2024 Dec;31(12):1625-1635. [Abstract]; The angiogenesis inhibitor Fruquintinib (Fq) (2 mg/kg; i.g.; once daily) treatment effectively attenuated fructose-induced development of MIA Paca2 cell xenograft tumor.

: Fruquintinib purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Nov 5:259:115703. [Abstract]; Representative photographs of tumors and quantification in each group from the HCT116 xenograft model after Fruquintinib (10 mg/kg; p.o) or vehicle treatment.

: Fruquintinib purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2023 Nov 5:259:115703. [Abstract]; Representative images and quantification of Ki67, CD68, FAK and E-cad. Fruquintinib (10 mg/kg; p.o) suppressed the proliferation (Ki67 stain) and migration (CD68, FAK, E-cad stain) of tumor cells from the HCT116 xenograft model.

: Fruquintinib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2023 Jun 18:661:10-20. [Abstract]; Fruquintinib (2.5 mg/kg; i.g.; once daily for 2 weeks) treatment resulted in slower growth and reduced volume of B16.F1-OVA tumors in C57BL/6 mice.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

View All Isoforms

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

Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC₅₀s of 33, 0.35, and 35 nM, respectively.

IC₅₀ & Target^[1]

VEGFR1

33 nM (IC₅₀)

VEGFR2

35 nM (IC₅₀)

VEGFR3

0.5 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	> 10 3 Compound: Fruquintinib	Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
COLO 205	IC₅₀	>10 3 Compound: Fruquintinib	Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HCT-116	IC₅₀	0.8 3 Compound: Fruquintinib	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HT-29	IC₅₀	1.5 3 Compound: Fruquintinib	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HCT-116	IC₅₀	0.8 3 Compound: Fruquintinib	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
LoVo	IC₅₀	>10 3 Compound: Fruquintinib	Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HT-29	IC₅₀	1.5 3 Compound: Fruquintinib	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
LoVo	IC₅₀	> 10 3 Compound: Fruquintinib	Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]

In Vitro

Fruquintinib demonstrates potent inhibition on VEGF-A dependent KDR phosphorylation in HEK293-KDR cells and VEGF-A induced proliferation in primary HUVECs with IC₅₀s of 0.6±0.2 nM and 1.7 nM, respectively. Similarly, potent VEGFR3 attenuation by fruquintinib is observed in primary HLECs, with IC₅₀s of 1.5 nM and 4.2 nM for VEGF-C stimulated VEGFR3 phosphorylation and proliferation, respectively. Fruquintinib suppresses the tube branching, tube length and area in a concentration-dependent manner. The tubule length of primary HUVECs decreased by 74% and 94% at 0.03 and 0.3 μM of fruquintinib, respectively. Fruquintinib inhibits HUVEC tubule growth and CAM angiogenesis. Tube formation is suppressed significantly after treatment with fruquintinib at 0.3 μM for 18 hours^[1].

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

In Vivo

Gastric cancer BGC-823 model is found to be most sensitive to fruquintinib. In this model, fruquintinib inhibits tumor growth by 62.3% and 95.4～98.6%, at 0.5 and 2 mg/kg once daily dosing, respectively. When the dose is elevated to 5 mg/kg and 20 mg/kg, the tumors regress by 24.1% and 48.6%, respectively. The level of anti-tumor growth activity of fruquintinib varies in different tumor xenograft models. Fruquintinib significantly decreases the micro-vessel density even at the lowest dose of 0.8 mg/kg^[1].

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

Clinical Trial

분자량

393.39

화학식

C₂₁H₁₉N₃O₅

CAS No.

1194506-26-7

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C)OC2=CC(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)=CC=C12)NC

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

용액&용해도

In Vitro:

DMSO : 5 mg/mL (12.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5420 mL	12.7100 mL	25.4201 mL
5 mM	0.5084 mL	2.5420 mL	5.0840 mL
10 mM	0.2542 mL	1.2710 mL	2.5420 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.33 mg/mL (0.84 mM); Clear solution

This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.33 mg/mL (0.84 mM); Clear solution

This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 0.33 mg/mL (0.84 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 0.33 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.98%

Select Batch:

Data Sheet (287 KB) SDS (396 KB)

COA (260 KB) HNMR (261 KB) RP-HPLC (221 KB) LCMS (100 KB)

Handling Instructions (2659 KB)

References

[1]. Sun Q, et al. Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45. [Content Brief]

Cell Assay ^[1]	Primary HUVECs or HLECs in exponential phase are suspended in 100 μL of RPMI-1640 media containing 0.5% FBS, and seeded at 5000 cell/well in 96-well plates pre-coated with 0.2% gelatin or fibronectin, and incubated overnight in a 5% CO₂, 37°C incubator. Fruquintinib and VEGF-A165 or VEGF-C (50 ng/mL) are added and incubated for 48 hours. Viability of the cells is determined using CCK-8 assay format^[1]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration ^[1]	Mice: The patient derived xenograft models are established after the primary tumor adopted serial passages in vivo. Once tumors have grown to 100-300 mm³, the animals are randomly assigned with 6-8 animals per group. The mice are treated orally with the vehicle (control group) or fruquintinib at a dose range of 0.5-20 mg/kg suspended in the vehicle (treated group) once daily for 3 weeks. In combination studies, docetaxel (Taxotere, 5 mg/kg) or oxaliplatin (10 mg/kg) is administered to nude mouse via intravenous injection, once a week. Tumor size and body weights are measured 3 times a week. Tumor volumes (TV) are calculated^[1]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
References	[1]. Sun Q, et al. Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5420 mL	12.7100 mL	25.4201 mL	63.5502 mL
	5 mM	0.5084 mL	2.5420 mL	5.0840 mL	12.7100 mL
	10 mM	0.2542 mL	1.2710 mL	2.5420 mL	6.3550 mL

Fruquintinib Related Classifications

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.

Keywords:

Fruquintinib1194506-26-7HMPL-013HMPL013HMPL 013VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

최근 본 상품:

상품명

Requested Quantity *

고객명 *

호칭

메일주소 *

전화번호 *

Department

회사명 *

City

도

Country or Region *

비고

상품명

Lot #

고객명 *

메일주소 *

전화번호

Department *

회사명 *

Country or Region *

비고

Name
이메일 *

	Sorry, but the email address you supplied was invalid.

Fruquintinib (Synonyms: HMPL-013)

고객리뷰

Other Forms of Fruquintinib:

Fruquintinib Related Antibodies

10 Publications Citing Use of MCE Fruquintinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

Biological Activity

Protocol

순도&문서

References

고객리뷰

Fruquintinib Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Fruquintinib Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report