LFM-A13

Cat. No.: HY-110002: FAQs
Data Sheet Handling Instructions

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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

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

LFM-A13 Chemical Structure

CAS No. : 62004-35-7

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5 mg	USD 150	Ask For Quote & Lead Time

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

Other Forms of LFM-A13:

(Z)-LFM-A13 In-stock

1 Publications Citing Use of MCE LFM-A13

•Nat Immunol. 2023 Nov;24(11):1813-1824. [Abstract]

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Biological Activity
Purity & Documentation
References
Customer Review

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)

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.

Molecular Weight

360.00

Formula

C₁₁H₈Br₂N₂O₂

CAS No.

62004-35-7

Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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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

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

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

LFM-A13 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:

LFM-A1362004-35-7Polo-like Kinase (PLK)BtkJAKBruton tyrosine kinaseJanus kinaseancertransgenic mouseDMBAcytokine signallingBreast cancercarcinogenicInhibitorinhibitorinhibit

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