| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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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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| ln Vitro |
In a dose-dependent manner, CEP-37440 (0-3000 nM; 0-192 h) inhibits the growth of IBC cells [1]. In FC-IBC02, SUM 190, and KPL4, CEP-37440 (1000 nM; 0-120 h) decreases phosphorylated FAK1 (Tyr 397) and keeps levels low over time[1]. To encourage CEP-37440 (0-3000 nM; Sup-M2 and Karpas-299 cells), dose-dependent induction was used.
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| ln Vivo |
In Sup-M2 xenograft protein SCID mice, CEP-37440 (3-55 mg/kg; sidewall bid and qd for 12 days) suppresses the formation of breast tumors [2]. In Sup-M2 xenograft mouse tumors, CEP-37440 (30 mg/kg; once lateral for 24 hours) suppresses tyrosine phosphorylation [2]. CEP-37440 (1-10 mg/kg; po and i.v.; CD-1 model, Sprague-Dawley (SD) form) has acceptable pharmacokinetic properties and suppresses FAK phosphorylation in nude CWR22 xenograft mice tumors (55 mg/kg; once lateral for 24 hours) [2].
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| Cell Assay |
cell viability assay [1]
Cell Types: FC-IBC02, KPL4, SUM190, MDA-IBC03 and SUM149 Cell Tested Concentrations: 0, 300, 1000, 2000 and 3000 nM Incubation Duration: 0. , 24, 48, 72, 96, 120, 144, 168 and 192 hrs (hours) Experimental Results: diminished proliferation of IBC cell lines by three-fifths at low concentrations. Proliferation is almost completely inhibited at a concentration of 3000 nM. Western Blot Analysis[1] Cell Types: FC-IBC02, SUM 190 and KPL4 Cell Tested Concentrations: 1000 nM Incubation Duration: 0, 48, 72, 96 and 120 hrs (hours) Experimental Results: Phospho-FAK1 in FC-IBC02, SUM190 diminished by half and KPL4 cells after 48 hrs (hours). |
| References |
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| Additional Infomation |
CEP-37440 has been used in trials studying the treatment of Solid Tumors.
ALK-FAK Inhibitor CEP-37440 is an orally available dual kinase inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and focal adhesion kinase (FAK), with potential antineoplastic activity. Upon administration, ALK-FAK inhibitor CEP-37440 selectively binds to and inhibits ALK kinase and FAK kinase. The inhibition leads to disruption of ALK- and FAK-mediated signal transduction pathways and eventually inhibits tumor cell growth in ALK- and FAK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; its dysregulation and gene rearrangements are associated with a variety of tumors. The cytoplasmic tyrosine kinase FAK, a signal transducer for integrins, is upregulated and constitutively activated in various tumor types; it plays a key role in tumor cell migration, proliferation, survival, and tumor angiogenesis. |
| Molecular Formula |
C30H38CLN7O3
|
|---|---|
| Molecular Weight |
580.12
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| Exact Mass |
579.272
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| CAS # |
1391712-60-9
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| PubChem CID |
71721648
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.648
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
41
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| Complexity |
819
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CNC(=O)C1=CC=CC=C1NC2=NC(=NC=C2Cl)NC3=C(C4=C(C[C@H](CCC4)N5CCN(CC5)CCO)C=C3)OC
|
| InChi Key |
BCSHRERPHLTPEE-NRFANRHFSA-N
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| InChi Code |
InChI=1S/C30H38ClN7O3/c1-32-29(40)23-7-3-4-9-25(23)34-28-24(31)19-33-30(36-28)35-26-11-10-20-18-21(6-5-8-22(20)27(26)41-2)38-14-12-37(13-15-38)16-17-39/h3-4,7,9-11,19,21,39H,5-6,8,12-18H2,1-2H3,(H,32,40)(H2,33,34,35,36)/t21-/m0/s1
|
| Chemical Name |
2-[[5-chloro-2-[[(6S)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl]amino]pyrimidin-4-yl]amino]-N-methylbenzamide
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| Synonyms |
CEP-37440; CEP 37440; CEP37440
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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 : ~100 mg/mL (~172.38 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.31 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 25.0 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: ≥ 2.5 mg/mL (4.31 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 25.0 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: ≥ 2.5 mg/mL (4.31 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 | 1.7238 mL | 8.6189 mL | 17.2378 mL | |
| 5 mM | 0.3448 mL | 1.7238 mL | 3.4476 mL | |
| 10 mM | 0.1724 mL | 0.8619 mL | 1.7238 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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