Linifanib (Synonyms: ABT-869; AL-39324)

Name: Linifanib
Brand: MedChemExpress
SKU: HY-50751
Rating: 5.0 (4 reviews)

Cat. No.: HY-50751 Purity: 98.89%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC₅₀s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.

For research use only. We do not sell to patients.

Linifanib Chemical Structure

CAS No. : 796967-16-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 385	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 715	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 1320	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Linifanib:

Linifanib-d₄ Get quote
Linifanib (GMP) Get quote

4 Publications Citing Use of MCE Linifanib

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PDGFR PDGFRβ PDGFRα

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Flt-1

3 nM (IC₅₀)

KDR

4 nM (IC₅₀)

PDGFRβ

66 nM (IC₅₀)

FLT3

4 nM (IC₅₀)

CSF-1R

3 nM (IC₅₀)

Kit

14 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	8343 nM Compound: Linifanib	Antiproliferative activity activity human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity activity human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 35863236]
EA.hy 926	IC₅₀	2.48 μM Compound: ABT-869	Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay Antiangiogenic activity in human EA.hy 926 cells measured after 24 hrs by MTT assay	[PMID: 32750566]
HepG2	IC₅₀	4001 nM Compound: Linifanib	Antiproliferative activity activity human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity activity human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 35863236]
HL-60	IC₅₀	7880 nM Compound: Linifanib	Antiproliferative activity against human HL-60 cells harboring wildtype FLT3 assessed as cell growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human HL-60 cells harboring wildtype FLT3 assessed as cell growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 35863236]
HUVEC	IC₅₀	40.11 μM Compound: Linifanib	Antiproliferative activity against HUVEC after 72 hrs by cell titer glo-based fluorescence assay Antiproliferative activity against HUVEC after 72 hrs by cell titer glo-based fluorescence assay	[PMID: 30121211]
HUVEC	IC₅₀	4920 nM Compound: Linifanib	Cytotoxicity against HUVEC cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay Cytotoxicity against HUVEC cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 35863236]
K562	GI₅₀	> 20 μM Compound: ABT-869, 4	Antiproliferation activity against human K562 cells expressing wild type BCR/ABL after 72 hrs by MTS method Antiproliferation activity against human K562 cells expressing wild type BCR/ABL after 72 hrs by MTS method	[PMID: 21708468]
K562	IC₅₀	6963 nM Compound: Linifanib	Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 35863236]
MCF7	IC₅₀	17.03 μM Compound: Linifanib	Antiproliferative activity against human MCF7 cells after 72 hrs by cell titer glo-based fluorescence assay Antiproliferative activity against human MCF7 cells after 72 hrs by cell titer glo-based fluorescence assay	[PMID: 30121211]
MOLM-13	GI₅₀	0.037 μM Compound: 3, ABT-869	Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay Cytotoxicity against human MOLM13 cells harboring mutant FLT3 after 72 hrs by MTS assay	[PMID: 23618709]
MOLM-13	GI₅₀	0.037 μM Compound: ABT-869, 4	Antiproliferation activity against human MOLM13 cells expressing FLT3 mutation assessed as cell viability after 72 hrs by MTS method Antiproliferation activity against human MOLM13 cells expressing FLT3 mutation assessed as cell viability after 72 hrs by MTS method	[PMID: 21708468]
MOLM-13	IC₅₀	19 nM Compound: Linifanib	Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 35863236]
MOLT-4	GI₅₀	6.7 μM Compound: ABT-869, 4	Antiproliferation activity against human MOLT4 after 72 hrs by MTS method Antiproliferation activity against human MOLT4 after 72 hrs by MTS method	[PMID: 21708468]
MV4-11	GI₅₀	0.04 μM Compound: ABT-869, 4	Antiproliferation activity against FLT3/ITD harboring human MV4-11 cells after 72 hrs by MTS method Antiproliferation activity against FLT3/ITD harboring human MV4-11 cells after 72 hrs by MTS method	[PMID: 21708468]
MV4-11	IC₅₀	0.69 μM Compound: Linifanib	Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo-based fluorescence assay Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo-based fluorescence assay	[PMID: 30121211]
MV4-11	IC₅₀	3.4 nM Compound: Linifanib	Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as cell growth inhibition measured after 72 hrs by CCK8 assay	[PMID: 35863236]
NIH3T3	IC₅₀	4 nM Compound: 17p, ABT-869	Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells by ELISA Inhibition of VEGF-induced human KDR phosphorylation in mouse 3T3 cells by ELISA	[PMID: 17343372]
RS4-11	GI₅₀	9.2 μM Compound: ABT-869, 4	Antiproliferation activity against human RS4:11 cells expressing wild type FLT3 after 72 hrs by MTS method Antiproliferation activity against human RS4:11 cells expressing wild type FLT3 after 72 hrs by MTS method	[PMID: 21708468]
Sf9	IC₅₀	0.005 μM Compound: ABT-869, 4	Inhibition of recombinant GST-tagged VEGFR2 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay Inhibition of recombinant GST-tagged VEGFR2 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay	[PMID: 21708468]
Sf9	IC₅₀	0.007 μM Compound: 3, ABT-869	Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis Inhibition of recombinant GST tagged VEGFR2 (789 to 1356) (unknown origin) transfected in insect sf9 cells after 120 mins by wallac counting analysis	[PMID: 23618709]
Sf9	IC₅₀	0.02 μM Compound: 3, ABT-869	Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis Inhibition of wild type GST tagged FLT3 kinase (567 to 993) (unknown origin) transfected in insect sf9 cells after 4 hrs by wallac counting analysis	[PMID: 23618709]
Sf9	IC₅₀	0.02 μM Compound: ABT-869, 4	Inhibition of GST-tagged FLT3 expressing wild type kinase domain expressed in Sf9 insect cells after 4 hrs by Kinase-Glo assay Inhibition of GST-tagged FLT3 expressing wild type kinase domain expressed in Sf9 insect cells after 4 hrs by Kinase-Glo assay	[PMID: 21708468]
Sf9	IC₅₀	0.037 μM Compound: ABT-869, 4	Inhibition of recombinant GST-tagged VEGFR1 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay Inhibition of recombinant GST-tagged VEGFR1 expressed in Sf9 insect cells after 120 mins by Kinase-Glo assay	[PMID: 21708468]
Sf9	IC₅₀	0.76 μM Compound: 3, ABT-869	Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis Inhibition of recombinant GST tagged Aurora A kinase (123 to 401) (unknown origin) transfected in insect sf9 cells after 90 mins by wallac counting analysis	[PMID: 23618709]
Sf9	IC₅₀	0.76 μM Compound: ABT-869, 4	Inhibition of recombinant GST-tagged Aurora A expressed in Sf9 insect cells after 90 mins by Kinase-Glo assay Inhibition of recombinant GST-tagged Aurora A expressed in Sf9 insect cells after 90 mins by Kinase-Glo assay	[PMID: 21708468]
U-937	GI₅₀	19 μM Compound: ABT-869, 4	Antiproliferation activity against human FLT3 gene-deficient U937 cells after 72 hrs by MTS method Antiproliferation activity against human FLT3 gene-deficient U937 cells after 72 hrs by MTS method	[PMID: 21708468]

In Vitro

Linifanib (0-10000 nM; 72 hours) inhibits in vitro the cell proliferation of 8305C and 8505C cell lines in a concentration-dependent manner^[3].
Linifanib significantly decreased the levels of phospho-CSF-1R after 24 h and 72 h in both 8505C and 8305C cells^[3].

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

Cell Viability Assay^[3]

Cell Line:	8305C and 8505C cells
Concentration:	0-10000 nM
Incubation Time:	72 hours
Result:	Inhibited the 8305C and 8505C cell proliferation with an IC50 of 0.7 nM and 123.7 nM, respectively.

In Vivo

The synergistic ATC antitumor activity of linifanib (10 mg/kg; p.o.; daily for 33 days)/Irinotecan combination significantly increases the survival of ATC affected mice and induces some complete responses^[3].

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

Animal Model:	Six-week-old CD nu/nu male mice (bearing 8505C ATC cells)^[3]
Dosage:	10 mg/kg
Administration:	P.o.; daily for 33 days
Result:	The combination of linifanib and irinotecan produced a greater survival result than either monotherapy, and resulted in a significant higher median survival of 100 days.

Clinical Trial

Molecular Weight

375.40

Formula

C₂₁H₁₈FN₅O

CAS No.

796967-16-3

Appearance

Solid

Color

White to gray

SMILES

O=C(NC1=CC=C(C2=C3C(N)=NNC3=CC=C2)C=C1)NC4=C(C=CC(C)=C4)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 13.16 mg/mL (35.06 mM; Need ultrasonic; 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	2.6638 mL	13.3191 mL	26.6383 mL
5 mM	0.5328 mL	2.6638 mL	5.3277 mL
10 mM	0.2664 mL	1.3319 mL	2.6638 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.

Molarity Calculator
Dilution Calculator

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: ≥ 1.32 mg/mL (3.52 mM); Clear solution

This protocol yields a clear solution of ≥ 1.32 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.2 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: ≥ 1.32 mg/mL (3.52 mM); Clear solution

This protocol yields a clear solution of ≥ 1.32 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.2 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: ≥ 1.32 mg/mL (3.52 mM); Clear solution

This protocol yields a clear solution of ≥ 1.32 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.2 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)

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(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.

Purity & Documentation

Purity: 99.28%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (253 KB) HNMR (192 KB) LCMS (356 KB)

Handling Instructions (2659 KB)

References

[1]. Albert DH, et al. Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther, 2006, 5(4), 995-1006. [Content Brief]

[2]. Monroig-Bosque PDC, et al. OncomiR-10b hijacks the small molecule inhibitor linifanib in human cancers. Sci Rep. 2018;8(1):13106. Published 2018 Aug 30. [Content Brief]

[3]. Banchi M, et al. Synergistic activity of linifanib and irinotecan increases the survival of mice bearing orthotopically implanted human anaplastic thyroid cancer. Am J Cancer Res. 2020;10(7):2120-2127. Published 2020 Jul 1. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.6638 mL	13.3191 mL	26.6383 mL	66.5956 mL
	5 mM	0.5328 mL	2.6638 mL	5.3277 mL	13.3191 mL
	10 mM	0.2664 mL	1.3319 mL	2.6638 mL	6.6596 mL
	15 mM	0.1776 mL	0.8879 mL	1.7759 mL	4.4397 mL
	20 mM	0.1332 mL	0.6660 mL	1.3319 mL	3.3298 mL
	25 mM	0.1066 mL	0.5328 mL	1.0655 mL	2.6638 mL
	30 mM	0.0888 mL	0.4440 mL	0.8879 mL	2.2199 mL

Linifanib Related Classifications

Help & FAQs

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Linifanib (Synonyms: ABT-869; AL-39324)

Customer Review

Other Forms of Linifanib:

4 Publications Citing Use of MCE Linifanib

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Linifanib (Synonyms: ABT-869; AL-39324)

Customer Review

Other Forms of Linifanib:

Linifanib Related Antibodies

4 Publications Citing Use of MCE Linifanib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PDGFR Isoform Specific Products:

View All VEGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Linifanib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Linifanib Related Classifications

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