Cat. No.: HY-110002

LFM-A13

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LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC₅₀s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research

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Pureté: 99.65%
CAS No.: 62004-35-7
Formule: C₁₁H₈Br₂N₂O₂
Masse moléculaire:360.00

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LFM-A13 Chemical Structure

CAS No.: 62004-35-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]^[3]

Plx1

10 μM (IC₅₀)

PLK3

61 μM (IC₅₀)

BRK

267 μM (IC₅₀)

BMX

281 μM (IC₅₀)

FYN

240 μM (IC₅₀)

Met

215 μM (IC₅₀)

Btk

2.5 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform Polo-like Kinase (PLK) :

Voir tous les produits spécifiques à Isoform JAK :

Cellular Effect

Cell Line	Type	Value	Description	References
Platelet	IC₅₀	2.8 μM Compound: 36	Inhibition of collagen-induced human platelet aggregation preincubated for 20 mins followed by collagen stimulation and measured for 10 mins by aggregometry Inhibition of collagen-induced human platelet aggregation preincubated for 20 mins followed by collagen stimulation and measured for 10 mins by aggregometry	[PMID: 32463237]
Sf21	IC₅₀	10.3 μM Compound: LFM-A13	Inhibition of xenopus recombinant Plx1 expressed in Sf21 cells by measuring autophosphorylation by 15-mins kinase assay Inhibition of xenopus recombinant Plx1 expressed in Sf21 cells by measuring autophosphorylation by 15-mins kinase assay	[PMID: 17098432]
Sf21	IC₅₀	32.5 μM Compound: LFM-A13	Inhibition of Xenopus recombinant Plx1 expressed in Sf21 cells by GST-Cdc25 substrate phosphorylation assay Inhibition of Xenopus recombinant Plx1 expressed in Sf21 cells by GST-Cdc25 substrate phosphorylation assay	[PMID: 17098432]

In Vitro

LFM-A13 (100 μM; 4 h) inhibits Epo-induced phosphorylation of EpoR, JAK2, BTK, STAT5, and ERK1/2 in R10 cells^[2].
LFM-A13 (100 μM; transfection 48 h) inhibits the autophosphorylation of JAK2, Tec and BTK in COS cells without affecting the autophosphorylation of Lyn kinase^[2].
LFM-A13 potently inhibits Plx1 with IC₅₀ of 10 μM; also inhibits BRK, BMX, FYN and Met with IC₅₀s of 267, 281, 240 and 215 μM, respectively^[3].

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

Cell Proliferation Assay^[3]

Cell Line:

PTK1 cells
Concentration:

100 µM
Incubation Time:

2 h
Result:

Significantly arrested cycle progression.

In Vivo

LFM-A13 (10 or 50 mg/kg; i.p.) exhibits anti-tumor effects dose dependently in the MMTV/Neu transgenic mouse model of breast cancer^[3]. FM-A13 (50 mg/kg; tiw; i.p.) attenuates DMBA-induced mammary tumorigenesis in mice by modulating a variety of factors associated with cell cycle, survival and apoptosis^[4].

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

Animal Model:

MMTV/neu transgenic mouse model^[3]
Dosage:

50 or 100 mg/kg
Administration:

Intraperitoneal injection (i.p.); twice a day for 5 consecutive days a week
Result:

Attenuated mammary tumor formation in mice.

Animal Model:

DMBA-induced breast cancer mouse model^[4]
Dosage:

50 mg/kg (or combinated with Paclitaxel (HY-B0015) (10 mg/kg; once per week intraperitoneally))
Administration:

Intraperitoneal injection (i.p.); 3 times a week
Result:

Inhibited DMBA-induced mammary tumor incidence, average tumor number, average tumor weight, and size in BALB/c mice.
Significantly decreased PLK1, cyclin D1, CDK-4, P53 and Bcl-2 expression, but increased the expression of p21, IκB, Bax and caspase 3 expression in mice.

Chemical Information

CAS No. 62004-35-7
Appearance Solid
Masse moléculaire 360.00
Formule C₁₁H₈Br₂N₂O₂
Color Off-white to light yellow
SMILES

C/C(O)=C(C#N)/C(NC1=CC(Br)=CC=C1Br)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (1)

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Journal Impact Factor

Nat Immunol

The ligation between ERMAP, galectin-9 and dectin-2 promotes Kupffer cell phagocytosis and antitumor immunity. [Abstract]

2023 Nov;24(11):1813-1824. PMID: 37813965

Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (694.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7778 mL

13.8889 mL

27.7778 mL

5 mM

0.5556 mL

2.7778 mL

5.5556 mL

10 mM

0.2778 mL

1.3889 mL

2.7778 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

LFM-A13 was dissolved in a solution containing 10% DMS0^[3]

Protocol 2

LFM-A13 was dissolved in a solution containing 15% DMS0^[4]

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (393 KB)
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- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Mahajan S, et al. Rational design and synthesis of a novel anti-leukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13 [alpha-cyano-beta-hydroxy-beta-methyl-N-(2, 5-dibromophenyl)propenamide]. J Biol Chem. 1999 Apr 2;274(14):9587-99. [Content Brief]

[2]. van den Akker E, et al. The Btk inhibitor LFM-A13 is a potent inhibitor of Jak2 kinase activity. Biol Chem. 2004 May;385(5):409-13. [Content Brief]

[3]. Uckun FM, et al. Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK). Bioorg Med Chem. 2007 Jan 15;15(2):800-14. [Content Brief]

[4]. Sahin K, et al. LFM-A13, a potent inhibitor of polo-like kinase, inhibits breast carcinogenesis by suppressing proliferation activity and inducing apoptosis in breast tumors of mice. Invest New Drugs. 2018 Jun;36(3):388-395. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7778 mL	13.8889 mL	27.7778 mL	69.4444 mL
	5 mM	0.5556 mL	2.7778 mL	5.5556 mL	13.8889 mL
	10 mM	0.2778 mL	1.3889 mL	2.7778 mL	6.9444 mL
	15 mM	0.1852 mL	0.9259 mL	1.8519 mL	4.6296 mL
	20 mM	0.1389 mL	0.6944 mL	1.3889 mL	3.4722 mL
	25 mM	0.1111 mL	0.5556 mL	1.1111 mL	2.7778 mL
	30 mM	0.0926 mL	0.4630 mL	0.9259 mL	2.3148 mL
	40 mM	0.0694 mL	0.3472 mL	0.6944 mL	1.7361 mL
	50 mM	0.0556 mL	0.2778 mL	0.5556 mL	1.3889 mL
	60 mM	0.0463 mL	0.2315 mL	0.4630 mL	1.1574 mL
	80 mM	0.0347 mL	0.1736 mL	0.3472 mL	0.8681 mL
	100 mM	0.0278 mL	0.1389 mL	0.2778 mL	0.6944 mL

Keywords

LFM-A13

1 Cited Publications

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LFM-A13

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

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Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LFM-A13

Voir tous les produits spécifiques à Isoform Polo-like Kinase (PLK)

Voir tous les produits spécifiques à Isoform JAK

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

LFM-A13 Related Classifications

HY-110002 Related Classifications