| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| Targets |
FLT3 WT (IC50 = 13 nM); FLT3 D835Y (IC50 = 8 nM)
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|---|---|
| ln Vitro |
FLT3-IN-3 (Compound 7d), at low nanomolar concentrations (GI50 values of 2 and 1 nM, respectively), very effectively inhibits the proliferation of FLT3-ITD positive MV4-11 and MOLM-13 cell lines[1].
FLT3-IN-3 (1 nM, 10nM, 100 nM, 1 μM and 10 μM; 72 hours) inhibits the Ba/F3 FLT3-ITD cells, and with a GI50 value of 1.136±0.389 μM, it inhibits the parental Ba/F3 cells with the GI50 value of 1.136±0.389 μM[1]. The FLT3 receptor tyrosine kinase can be prevented from autophosphorylating at three distinct tyrosine residues (589, 591, and 842) at concentrations as low as 1 nM. Additionally, several downstream targets of FLT3 are suppressed from being phosphorylated by this inhibition. Notably, FLT3-IN-3 (0.01, 0.1, 1, 10 and 100 nM; 1 hour) eliminates the direct substrate of the oncogenic FLT3-ITD variant, Y694, which phosphorylates STAT5. The MAPK cascade is the other pathway impacted. Treatment with FLT3-IN-3 results in decreased phosphorylation of two important signaling pathway components: MEK1/2 (S217/221) and ERK1/2 (T202/Y204). AKT's decreased phosphorylation at S473 indicates that FLT3-IN-3 also interferes with the PI3K/AKT pathway[1]. |
| ln Vivo |
In mice undergoing subcutaneous MV4-11 xenografts, a single dose of FLT3-IN-3 (Compound 7d; 10 mg/kg; i.p.) results in a 48-hour sustained inhibition of FLT3 and STAT5 phosphorylation[1].
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| Cell Assay |
Cell Line: Murine Ba/F3 FLT3-ITD and parental Ba/F3 cells
Concentration: 1 nM, 10nM, 100 nM, 1 μM and 10 μM Incubation Time: 72 hours Result: The GI50s for Ba/F3 FLT3-ITD cells and parental Ba/F3 cells are 0.034±0.015 μM and 1.136±0.389 μM, respectively. |
| Animal Protocol |
Female athymic nu/nu mice with subcutaneously implanted MV4-11 xenografts
10 mg/kg Intraperitoneal (i.p.) injection; 48 hours |
| References |
| Molecular Formula |
C27H38N8O
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|---|---|
| Molecular Weight |
490.6436
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| Exact Mass |
490.32
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| Elemental Analysis |
C, 66.09; H, 7.81; N, 22.84; O, 3.26
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| CAS # |
2229050-90-0
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| Related CAS # |
2229050-90-0
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| PubChem CID |
133081975
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| Appearance |
White to off-white solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
36
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| Complexity |
671
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SAEGVASGMTZGFI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H38N8O/c28-20-7-11-22(12-8-20)31-27-32-25(24-26(33-27)35(18-29-24)23-3-1-2-4-23)30-21-9-5-19(6-10-21)17-34-13-15-36-16-14-34/h5-6,9-10,18,20,22-23H,1-4,7-8,11-17,28H2,(H2,30,31,32,33)
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| Chemical Name |
2-N-(4-aminocyclohexyl)-9-cyclopentyl-6-N-[4-(morpholin-4-ylmethyl)phenyl]purine-2,6-diamine
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| Synonyms |
SAN50900; SAN 50900; SAN-50900; FLT3-IN3; FLT3-IN 3; FLT3-IN-3
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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: ~250 mg/mL (~509.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0382 mL | 10.1908 mL | 20.3815 mL | |
| 5 mM | 0.4076 mL | 2.0382 mL | 4.0763 mL | |
| 10 mM | 0.2038 mL | 1.0191 mL | 2.0382 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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