| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
FLT3-IN-2 targets FLT3 with an IC50 of less than 1 μM. By inhibiting FLT3, it blocks the downstream signaling pathways that promote the proliferation and survival of hematopoietic cells, making it a potential therapeutic target for acute myeloid leukemia (AML) and other hematological malignancies.
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|---|---|
| ln Vitro |
In vitro, FLT3-IN-2 demonstrates potent inhibition of FLT3 kinase activity with an IC50 of less than 1 μM. Its activity is confirmed in cell-based assays where it inhibits the proliferation of FLT3-dependent cell lines.
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| ln Vivo |
In vivo, FLT3-IN-2 supports the development of targeted therapies and advances research in cancer biology. As a FLT3 inhibitor, it has potential for the treatment of acute myeloid leukemia (AML) and other hematological malignancies.
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| Enzyme Assay |
The in vitro FLT3 kinase assay involves incubating the enzyme with a peptide substrate and ATP in the presence of varying concentrations of FLT3-IN-2. The amount of phosphorylated substrate is measured using a luminescent or fluorescent detection system, and the IC50 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cell-based assays for FLT3-IN-2 utilize FLT3-dependent cell lines, such as MV4-11 or MOLM-13. Cells are treated with the compound, and cell viability is assessed by MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal experiments for FLT3-IN-2 would typically involve xenograft models using FLT3-dependent human leukemia cells. The compound would be administered orally or intraperitoneally, and tumor growth would be monitored.
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| ADME/Pharmacokinetics |
FLT3-IN-2 has a molecular weight of 416.83 g/mol and is soluble in DMSO at 30 mg/mL. It is typically stored as a powder at -20°C. For in vivo studies, it can be formulated in suitable vehicles.
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| Toxicity/Toxicokinetics |
Toxicological data for FLT3-IN-2 are limited, as it is a research compound. It is not intended for human use. Standard safety precautions for handling chemical reagents should be followed.
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| References | |
| Additional Infomation |
FLT3-IN-2 is a research compound with no clinical approval. It is a valuable tool for studying FLT3 biology and the role of FLT3 in hematological malignancies. It is used in drug discovery programs to explore the therapeutic potential of FLT3 inhibitors for the treatment of acute myeloid leukemia.
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| Molecular Formula |
C₂₁H₁₆CLF₃N₄
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|---|---|
| Molecular Weight |
416.83 Synonym
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| Exact Mass |
416.101
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| CAS # |
923562-23-6
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| PubChem CID |
59593294
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.658
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| LogP |
5.86
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
527
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1CNC2=NC=C(C=C2)CC3=CNC4=C3C=C(C=N4)Cl)C(F)(F)F
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| InChi Key |
MFXPJGJSKHZZGC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H16ClF3N4/c22-17-8-18-15(11-28-20(18)29-12-17)7-14-3-6-19(27-10-14)26-9-13-1-4-16(5-2-13)21(23,24)25/h1-6,8,10-12H,7,9H2,(H,26,27)(H,28,29)
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| Chemical Name |
5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[4-(trifluoromethyl)phenyl]methyl]pyridin-2-amine
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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) |
DMSO : ≥ 30 mg/mL (~71.97 mM)
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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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