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| 50mg |
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| Targets |
eCF506 targets Src tyrosine kinase, a member of the Src family of kinases (SFKs). Src kinases are key regulators of cancer cell proliferation, migration, and survival. eCF506 is a highly selective Src inhibitor. It locks Src into its native "closed" conformation, inhibiting both kinase activity and protein-protein interactions.
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| ln Vitro |
In MCF7 and MDA-MB-231 cells, eCF506 has extremely strong anti-apoptotic effects. SRC and FAK phosphorylation is inhibited by eCF506 at low nanomolar concentrations; total inhibition is shown at 100 nM. The study found that eCF506 at 10 nM dramatically inhibited cell motility as early as 6 hours in, which is comparable to the effect of dasatinib. With IC50 values for SRC and YES that are subnanomolar (IC50=0.5, 2.1 nM), eCF506 exclusively inhibits SFK. It should be noted that the primary target in ABL, SRC, has a significant difference in activity (>950-fold difference) in eCF506 [1].
In vitro, eCF506 potently inhibits Src tyrosine kinase with an IC50 of <0.5 nM. It is a highly selective inhibitor. The compound inhibits the growth and proliferation of cancer cells by inducing apoptosis and suppressing tumor growth. Its ability to lock Src into a "closed" conformation distinguishes it from other Src inhibitors. |
| ln Vivo |
eCF506 has a 25.3% bioavailability, which is moderate. When comparing eCF506-treated xenograft slices to untreated animal controls, a notable decrease in phospho-SRCY416 was seen [1].
In vivo, eCF506 is orally bioavailable. It has potential applications in oncology research. By inhibiting Src signaling, it suppresses tumor growth and proliferation. The compound's oral bioavailability supports its use in in vivo efficacy studies. Further preclinical studies would evaluate its antitumor activity in xenograft models. |
| Enzyme Assay |
In vitro kinase assays for eCF506 measure Src kinase inhibition using recombinant Src enzyme. Kinase activity is assessed by measuring phosphorylation of a peptide substrate using radiometric (³³P-ATP) or fluorescence-based methods. Various concentrations of eCF506 are added. IC50 values are calculated from dose-response curves. Selectivity profiling against a panel of kinases is performed to assess specificity.
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| Cell Assay |
Cellular assays for eCF506 use cancer cell lines. Cells are treated with various concentrations of eCF506. Src phosphorylation is assessed by Western blotting using phospho-specific Src antibodies. Cell proliferation is measured using MTT or ATP-lite assays. Apoptosis is assessed by caspase-3/7 activity or Annexin V staining. These assays confirm the compound's activity.
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| Animal Protocol |
In vivo animal studies for eCF506 utilize tumor xenograft models in mice. The compound is administered orally at various doses. Tumor volume is measured over time. Src phosphorylation and downstream signaling are assessed in tumor tissue. Apoptosis markers are evaluated. Efficacy is compared to vehicle and reference Src inhibitors. Pharmacokinetic sampling is performed to correlate exposure with efficacy.
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| ADME/Pharmacokinetics |
eCF506 has molecular weight of 510.63 g/mol and molecular formula C26H38N8O3. Purity is >98%. It is typically stored as powder at -20°C for up to 3 years. It is soluble in DMSO. It is orally bioavailable. Pharmacokinetic properties support once-daily oral dosing.
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| Toxicity/Toxicokinetics |
Preclinical toxicity of eCF506 has not been extensively documented. As a Src kinase inhibitor, potential adverse effects may include gastrointestinal effects, skin rash, and fatigue, which are class effects of tyrosine kinase inhibitors. Standard toxicology studies would be required for therapeutic development. Safety pharmacology would assess cardiovascular, respiratory, and CNS effects.
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| References | |
| Additional Infomation |
eCF506 (NXP900) is a highly potent and selective Src tyrosine kinase inhibitor with an IC50 of <0.5 nM. It locks Src into a "closed" conformation. It has potential applications in oncology research. It is available for research purposes only.
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| Molecular Formula |
C26H38N8O3
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| Molecular Weight |
510.63
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| Exact Mass |
510.306
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| CAS # |
1914078-41-3
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| PubChem CID |
121231408
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| Appearance |
White to yellow solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
37
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| Complexity |
742
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=C(C=CC(NC(=O)OC(C)(C)C)=C1OC)C1=NN(CCN2CCC(CC2)N(C)C)C2N=CN=C(N)C1=2
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| InChi Key |
GMPQGWXPDRNCBL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H38N8O3/c1-26(2,3)37-25(35)30-19-8-7-17(15-20(19)36-6)22-21-23(27)28-16-29-24(21)34(31-22)14-13-33-11-9-18(10-12-33)32(4)5/h7-8,15-16,18H,9-14H2,1-6H3,(H,30,35)(H2,27,28,29)
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| Chemical Name |
tert-butyl N-[4-[4-amino-1-[2-[4-(dimethylamino)piperidin-1-yl]ethyl]pyrazolo[3,4-d]pyrimidin-3-yl]-2-methoxyphenyl]carbamate
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| Synonyms |
eCF 506; eCF-506; eCF506
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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 : ~62.5 mg/mL (~122.40 mM)
H2O : ~0.1 mg/mL (~0.20 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.07 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 (4.07 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 (4.07 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 | 1.9584 mL | 9.7918 mL | 19.5837 mL | |
| 5 mM | 0.3917 mL | 1.9584 mL | 3.9167 mL | |
| 10 mM | 0.1958 mL | 0.9792 mL | 1.9584 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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