| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
IMC-EB10 (10 μg/mL, 1 h) reduced phosphorylation of FLT3 and its downstream signaling proteins STAT5, Akt and MAPK in Hb1119 and SEM-K2 cells, but activated these proteins in REH and RS411 cells [1]. IMC-EB10 (10 μg/mL, 1 h) activated FLT3 and its downstream Akt in ALLs [1]. IMC-EB10 (0.4-200 nM, 1 h) inhibited FLT3-Fc-induced phosphorylation of wild-type FLT3 and ligand-independent constitutive phosphorylation of ITD mutant FLT3 in EOL-1, EM3, BaF3-ITD and MV4;11 cells [4]. IMC-EB10 (0.4-200 nM, 1 h) inhibited FLT3-Fc-induced phosphorylation of MAPK, AKT, and Stat5 in EOL-1, EM3, BaF3-ITD, and MV4;11 cells[4]. IMC-EB10 (1.5-100 nM, 1 h) inhibited FLT3-Fc-induced proliferation of EOL-1 and BaF3-ITD cells[4].
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| ln Vivo |
IMC-EB10 (400 μg/10 mg/kg, intraperitoneal injection, three times a week starting 24 hours after cell injection / once a day starting 24 hours after cell injection / three times a day starting 7 days after cell injection for a total of 30 days / twice a week for a total of 3 weeks) can simplify the presence of SEM-K2 cells in the SEM-K2 NOD/SCID model, induce cytotoxicity through natural killer cells, do not select cells, and prolong survival compared with methotrexate alone [1][3]. IMC-EB10 (400 μg, intraperitoneal injection, three times a week for a total of 14 weeks) can reduce cell entry in the ALLs NOD/SCID model [1]. IMC-EB10 (100-500 μg, intraperitoneal injection, three times a week for a total of 14 weeks). IMC-EB10 (100-500 μg, intraperitoneal injection, three times a week for a total of 14 weeks). In 20-day EOL-1 and BaF3-ITD xenograft leukocyte models, the number of cells in the bone marrow was reduced and the survival of tumors was prolonged[4].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Hb1119, SEM-K2 cells Tested Concentrations: 10 μg/mL Incubation Duration: 1 h Experimental Results: Reduced FLT3 and phosphorylation of downstream signaling proteins STAT5, Akt, and MAPK. Western Blot Analysis[1] Cell Types: REH, RS411 cells Tested Concentrations: 10 μg/mL Incubation Duration: 1 h Experimental Results: Activated FLT3 and phosphorylation of downstream signaling proteins STAT5, Akt, and MAPK. Western Blot Analysis[1] Cell Types: ALLs Tested Concentrations: 10 μg/mL Incubation Duration: 1 h Experimental Results: Activated FLT3 and downstream Akt. ELISA Assay[4] Cell Types: EOL-1, EM3, BaF3-ITD, MV4;11 cells Tested Concentrations: 0.1, 0.4, 1, 4, 10, 40, 100, 200 nM Incubation Duration: 1 h Experimental Results: Blocked FL-induced FLT3 receptor phosphorylation in a dose dependent manner with an IC50 of 0.4 to 4 nM. Blocked the phosphorylation and constitutive phosphorylation of MAPK, inhibited FL-induced phosphorylation of AKT and Stat5 phosphorylation in EOL-1 and BaF3-ITD cells. |
| Animal Protocol |
Animal/Disease Models: SEM-K2 (0.5×106) NOD/SCID mice model[1]
Doses: 400 μg Route of Administration: i.p., thrice per week starting 24 hours after cell injection/once starting 24 hours after cell injectio total of thrice every other day starting 24 hours after cell injection or thrice per week starting 7 days after cell injection, 30 days Experimental Results: Reduced human cells in peripheral blood, spleen, and bone marrow, reducing the presence of SEM-K2 cells to <1%, prolonged survival. Did not select for resistant cells, mediated cytotoxicity through natural killer cells. Animal/Disease Models: ALLs (1×106) NOD/SCID mice model[1] Doses: 400 μg Route of Administration: i.p., three times a week, 14 weeks Experimental Results: Reduced cell implantation. Animal/Disease Models: SEM-K2 (5×105) NOD/SCID mice model[3] Doses: 10 mg/kg + 100 mg/kg Methotrexate Route of Administration: i.p., 2×/week, 3 weeks + once per week for 3 weeks Experimental Results: Significantly prolonged survival compared to Methotrexate alone. Animal/Disease Models: EOL-1 (5×106) xenograft leukemia NOD/SCID mice (male, , 6-8 weeks) model[4] Doses: 100, 250, 500 μg Route of Administration: i.p., 3 times weekly, 20 days Experimental Results: Decreased the number of tumor cells in bone marrow. Animal/Disease Models: BaF3-ITD (5×104) xenograft leukemia NOD/SCID mice (male, , 6-8 weeks) model[4] Doses: 100, 500 μg Route of Administration: i.p., 3 times weekly Experimental Results: Prolonged the survival. |
| References |
| Appearance |
Typically exists as solids at room temperature
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| Synonyms |
LY3012218
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| HS Tariff Code |
2934.99.9001
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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 Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
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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