| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
FLT3 (FMS-like tyrosine kinase 3). FLT3-IN-19 is a potent and selective FLT3 inhibitor that binds to the ATP-binding pocket, blocking FLT3 activation and downstream signaling pathways involved in cell proliferation and survival in AML.
|
|---|---|
| ln Vitro |
FLT3-IN-19 inhibits FLT3 with an IC50 of 0.213 nM, demonstrating extremely high potency. It is a potent and selective FLT3 inhibitor suitable for AML disease research. Its high potency suggests it can effectively block FLT3 signaling at low nanomolar concentrations, leading to reduced cell proliferation and increased apoptosis in FLT3-driven cells.
|
| ln Vivo |
No specific in vivo activity data are reported for FLT3-IN-19. As a highly potent FLT3 inhibitor, it is expected to have strong anti-tumor activity in AML xenograft models driven by FLT3 mutations. Its selectivity and potency make it a valuable tool for studying FLT3-dependent pathways and potential therapeutic interventions.
|
| Enzyme Assay |
Cell-free FLT3 kinase assays are performed using recombinant human FLT3 enzyme. The compound is incubated with the enzyme and a peptide substrate in the presence of ATP for 30-60 minutes. Kinase activity is measured using a luminescence-based ADP detection kit. IC50 (0.213 nM) is determined from a dose-response curve using nonlinear regression.
|
| Cell Assay |
FLT3-mutant human AML cell lines (e.g., MV4-11, MOLM-13) are seeded in 96-well plates and treated with increasing concentrations of FLT3-IN-19 for 72 hours. Cell viability is assessed using the MTT assay or CellTiter-Glo reagent. FLT3 phosphorylation and downstream signaling (p-STAT5, p-ERK) are measured by Western blotting. Apoptosis is measured by Annexin V/PI staining.
|
| Animal Protocol |
For in vivo studies, FLT3-IN-19 would be administered orally to mice bearing FLT3-mutant AML xenografts. Dosing is typically once or twice daily for 2-4 weeks. Tumor volumes are measured with calipers. At study termination, tumors are excised for pharmacodynamic analysis of FLT3 phosphorylation and downstream signaling. No published studies are available.
|
| ADME/Pharmacokinetics |
No specific PK data are reported for FLT3-IN-19. The molecular weight is 418.49 (C22H26N8O). CAS 2237234-48-7. It is soluble in DMSO (10-50 mg/mL). For in vivo studies, it would typically be formulated in 0.5% methylcellulose. Oral bioavailability, half-life, and other PK parameters have not been characterized.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are reported for FLT3-IN-19. As a highly potent FLT3 inhibitor, potential on-target toxicity may include myelosuppression. Comprehensive toxicological assessments have not been published. The compound is for research use only and is not an FDA-approved drug.
|
| References | |
| Additional Infomation |
Other information: FLT3-IN-19 (CAS 2237234-48-7) is a research compound and not FDA-approved. It is a potent and selective FLT3 inhibitor with an IC50 of 0.213 nM. It is a valuable tool for studying acute myeloid leukemia (AML) and FLT3-dependent signaling pathways. Purity ≥98%. For research use only. Synonyms: FLT3-IN-19, Comp 50.
|
| Molecular Formula |
C22H26N8O
|
|---|---|
| Molecular Weight |
418.494843006134
|
| Exact Mass |
418.222
|
| CAS # |
2237234-48-7
|
| PubChem CID |
145957309
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
2.6
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
31
|
| Complexity |
606
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=NC2=C(CCC2)C(=N1)NC3=C(NN=C3)C(=O)NC4=CC=C(C=C4)N5CCNCC5
|
| InChi Key |
DXUDRTZDTCQOLU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H26N8O/c1-14-25-18-4-2-3-17(18)21(26-14)28-19-13-24-29-20(19)22(31)27-15-5-7-16(8-6-15)30-11-9-23-10-12-30/h5-8,13,23H,2-4,9-12H2,1H3,(H,24,29)(H,27,31)(H,25,26,28)
|
| Chemical Name |
4-[(2-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)amino]-N-(4-piperazin-1-ylphenyl)-1H-pyrazole-5-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3895 mL | 11.9477 mL | 23.8954 mL | |
| 5 mM | 0.4779 mL | 2.3895 mL | 4.7791 mL | |
| 10 mM | 0.2390 mL | 1.1948 mL | 2.3895 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
