| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
FLT3-IN-15 (Compound 36) (0-100 nM) has anti-proliferative action on MOLM14 cell line [1], with concentrations ranging from 0 to 100 nM. The FLT3-IN-15 (0-1 μM; 72 hours) demonstrates an excellent safety profile against different cancer cell lines and is more sensitive to MV4-11 cells than the K562 cell line [1]. In MV4-11 cells, FLT3-IN-15 (0.01-1 μM; 4 hours) potently inhibits the phosphorylation of Erk1/2 and STAT5 [1].
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| ln Vivo |
In all mice, FLT3-IN-15 (20 mg/kg; oral; once daily for 21 days) resulted in a swift and total tumor remission [1]. One female mouse died on day 6 from FLT3-IN-15 (2000 mg/kg; oral; single dose); the female's estimated LD50 was 4,950 mg/kg [1]. According to reference [1], FLT3-IN-15 (10 μM) inhibits hERG ligand binding by 21.4%. FLT3-IN-15 (10 mg/kg; oral and intravenous injection; single dose) exhibits a 42.6% significant increase in oral bioavailability, an AUClast of 25.0 μg·min/mL, and a Cmax of 36.5 ng/mL. FLT3-IN-15 pharmacokinetic parameters in male ICR mice [1]. PO (10 mg/kg) IV (10 mg/kg) AUClast (μg·min/mL) 25.0 ± 11.6 58.5 ± 57.4 AUCinf (μg·min/mL) 62.1 ± 58.6 103.4 ± 95.3 MRT (hr) 2811.3 ± 2713.0 1257.1 ± 1084.1 T1/2 (hour) 1775.7 ± 1901.0 1099.2 ± 98.7 VSS (L/kg) 127891 ± 104764 Cmax (ng/mL) 36.5 ± 24.3 Tmax (min) 390.0 ± 366.0 Xu, 24h (%) 0.001 ± 0.0 0.002 GI24h (%) 0.05 ± 0.24 ± 0.02 F (%) 42.9
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| Cell Assay |
Cell Proliferation Assay
Cell Types: MOLM14 wild-type cells, MOLM14-ITD cells, MOLM14-ITD-D835Y cells, MOLM14-ITD-F691L cells [1] Tested Concentrations: 0-100 nM Incubation Duration: Experimental Results: Demonstrated anti-proliferation against MOLM14 Active cell lines, GI50 in MOLM14 wild-type cells, MOLM14-ITD cells, MOLM14-ITD-D835Y cells and MOLM14-ITD-F691L cells are 4.88±0.67nM, 1.85±0.06nM, 1.87±0.36nM and 3.27±0.99nM ,respectively. Cell proliferation assay Cell Types: MV4-11, K562, A549, HepG2, MDA-MB-231, HCT-116, PC3 and SK-OV-3[1] Tested Concentrations: 0-1 μM Incubation Duration: 72 hrs (hours) Experimental Results: Displayed It is extremely sensitive to MV4-11 cells (GI50 = 1 nM) compared to the K562 cell line and exhibits a good safety profile against other cancer cell lines. Western Blot Analysis Cell Types: MV4-11[1] Tested Concentrations: 10 nM, 100 nM and 1 μM Incubation Duration: 4 hrs (hours) Experimental Results: Demonstrated strong blockade of STAT5 and Erk1/2 phosphorylation. |
| Animal Protocol |
Animal/Disease Models: BALB/c nu/nu (injection of MV4-11) [1]
Doses: 20 mg / kg Route of Administration: PO; one time/day for 21 days Experimental Results: All mice experienced rapid and complete tumor response and no weight loss or any other signs of toxicity during dosing. Animal/Disease Models: Female ICR mice [1] Doses: 2000 mg/kg Route of Administration: Oral; Single Experimental Results:Caused death of one female mouse in the 2,000 mg/kg group on day 6, and determined the death of the male mouse The approximate lethal dose (ALD) exceeded 2,000 mg/kg and 2,000 mg/kg for female mice respectively; the LD50 value for female mice was calculated to be 4,950 mg/kg. Animal/Disease Models: Male ICR mouse[1] Doses: 10 mg/kg Route of Administration: oral and intravenous (iv) (iv)injection; single (pharmacokinetic/PK/PK analysis) Experimental Results: AUClast is 25.0 μg·min/mL, Cmax is 36.5 ng/mL , the oral bioavailability was Dramatically increased by 42.6%. |
| References |
| Molecular Formula |
C22H23CLFN5O2
|
|---|---|
| Molecular Weight |
443.901726961136
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| Exact Mass |
443.152
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| CAS # |
2435562-99-3
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| PubChem CID |
162670691
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| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
668
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CCN1)CCO/N=C/2\C3=CC=CC=C3N=C2C4=C(NC5=C4C=C(C=C5)F)O.Cl
|
| InChi Key |
FYOZPHRPSXFBMH-PQAWYCKWSA-N
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| InChi Code |
InChI=1S/C22H22FN5O2.ClH/c23-14-5-6-18-16(13-14)19(22(29)26-18)21-20(15-3-1-2-4-17(15)25-21)27-30-12-11-28-9-7-24-8-10-28;/h1-6,13,24,26,29H,7-12H2;1H/b27-20+;
|
| Chemical Name |
5-fluoro-3-[(3E)-3-(2-piperazin-1-ylethoxyimino)indol-2-yl]-1H-indol-2-ol;hydrochloride
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2528 mL | 11.2638 mL | 22.5276 mL | |
| 5 mM | 0.4506 mL | 2.2528 mL | 4.5055 mL | |
| 10 mM | 0.2253 mL | 1.1264 mL | 2.2528 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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