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| 100mg | ||
| 250mg | ||
| 500mg |
LFM-A13 is a novel and potent inhibitor of BTK, JAK2, PLK with anticancer effects. It inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM.
| ln 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; transfected 48 h) inhibits COS cells. LFM-A13 effectively inhibits Plx1 with an IC50 of 10 μM. It also inhibits BRK, BMX, FYN and Met with an IC50 of 267 respectively.Cell lines : PTK1 cell concentration: 100 μM Incubation time: 2 h Results: Significantly inhibited cycle progression. 281, 240 and 215 μM[3].
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| ln Vivo |
LFM-A13 (10 or 50 mg/kg; intraperitoneal injection) revealed dose-dependent anti-tumor effects in the MMTV/Neu treatment regimen [3]. FM-A13 (50 mg/kg; three times a week; intraperitoneal injection) can reduce DMBA-induced mammary gland growth in mice via modulating a number of cell cycle, persistence and associated variables [4].
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| Cell Assay |
Cell proliferation assay [3]
Cell Types: PTK1 cell Tested Concentrations: 100 μM Incubation Duration: 2 h Experimental Results: Dramatically inhibited cycle progression. 281, 240 and 215 μM[3]. |
| Animal Protocol |
Animal/Disease Models: MMTV/neu transgenic mouse model [3]
Doses: 50 or 100 mg/kg Route of Administration: intraperitoneal (ip) injection; twice a day, 5 days a week. Experimental Results: Reduce the formation of mammary gland tumors in mice. Animal/Disease Models: DMBA-induced breast cancer mouse model [4] Doses: 50 mg/kg (or combined with paclitaxel (10 mg/kg; intraperitoneal (ip) injection once a week)) Route of Administration: intraperitoneal (ip) injection; weekly 3 Experimental Results: Inhibition of DMBA-induced mammary tumor incidence, average tumor number, average tumor weight and size in balb/c (Bagg ALBino) mouse. Dramatically diminished the expression of PLK1, cyclin D1, CDK-4, P53 and Bcl-2, but increased the expression of p21, IκB, Bax and caspase 3 in mice. |
| 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.
[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. [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. [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. |
| Molecular Formula |
C11H8N2O2BR2
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|---|---|
| Molecular Weight |
360.00142
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| CAS # |
62004-35-7
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| Related CAS # |
(Z)-LFM-A13;244240-24-2
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| SMILES |
C(/C(=C(\O)/C)/C(NC1C=C(Br)C=CC=1Br)=O)#N
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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