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Purity: ≥98%
W-7 HCl is a novel, potent and selective calmodulin antagonist with antitumor activity. It inhibits Ca2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively. W-7 hydrochloride induces apoptosis.
| ln Vitro |
W-7 is mostly found in the cytoplasm and prevents Chinese hamster ovary K1 (CHO-K1) cells from proliferating. W-7 acts in a specific manner to selectively block the G1/S border phase of the cell cycle. Cell growth at the G1/S border phase of the cell cycle can be inhibited by 25 μM W-7 [1]. The degree of antagonism between the contractile responses to KCl and carbachol is similar in W-7 (100 μM). Ten micrograms of carbachol stimulates myosin light chain (P-LC) phosphate level for one minute, while W-7 blocks this increase. By preventing the early rise in P-LC phosphorylation, W-7 inhibits smooth muscle contraction [2]. Multiple human multiple myeloma cell lines exhibit a dose-dependent reduction of cell growth upon treatment with W-7. W-7 upregulates p21cip1 and downregulates cyclins to cause G1 phase cell cycle arrest. W-7 activates caspase to cause apoptosis; this is partially achieved by raising intracellular calcium levels, depolarizing the mitochondrial membrane potential, inhibiting STAT3 phosphorylation, and subsequently downregulating the Mcl-1 protein [3]. With a Ki value of 300 μM, W-7 competitively inhibits phosphodiesterase that is dependent on Ca2+ and calmodulin [4].
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| ln Vivo |
In the mouse model of multiple myeloma, W-7 (3 mg/kg; intraperitoneal injection; 5 consecutive days per week; female BALB/c nu mice) therapy dramatically inhibited tumor growth [3].
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| Animal Protocol |
Animal/Disease Models: Female BALB/c nu (nude) mice (6 weeks old) were injected with RPMI 8226 cells [3]
Doses: 3 mg/kg Route of Administration: intraperitoneal (ip) injection; 5 days per week Experimental Results: significant in mouse MM model Reduce tumor growth. |
| References |
[1]. H Hidaka, et al. N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide, a Calmodulin Antagonist, Inhibits Cell Proliferation. Proc Natl Acad Sci U S A. 1981 Jul;78(7):4354-7.
[2]. M Asano. Divergent Pharmacological Effects of Three Calmodulin Antagonists, N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7), Chlorpromazine and Calmidazolium, on Isometric Tension Development and Myosin Light Chain Phosphorylation in Intact Bovin [3]. H Itoh, et al. Direct Interaction of Calmodulin Antagonists With Ca2+/calmodulin-dependent Cyclic Nucleotide Phosphodiesterase. J Biochem. 1984 Dec;96(6):1721-6. [4]. Shigeyuki Yokokura, et al. Calmodulin Antagonists Induce Cell Cycle Arrest and Apoptosis in Vitro and Inhibit Tumor Growth in Vivo in Human Multiple Myeloma. BMC Cancer. 2014 Nov 26;14:882. |
| Molecular Formula |
C16H22CL2N2O2S
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|---|---|
| Molecular Weight |
377.3291
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| CAS # |
61714-27-0
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| Related CAS # |
W-7 isomer hydrochloride;69762-85-2
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| SMILES |
O=S(C1=C2C=CC=C(Cl)C2=CC=C1)(NCCCCCCN)=O.[H]Cl
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| InChi Key |
OMMOSRLIFSCDBL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H21ClN2O2S.ClH/c17-15-9-5-8-14-13(15)7-6-10-16(14)22(20,21)19-12-4-2-1-3-11-18/h5-10,19H,1-4,11-12,18H21H
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| Chemical Name |
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide hydrochloride
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| Synonyms |
W-7 HCl W 7 HCl W7 HCl W-7 hydrochloride
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~662.55 mM)
H2O : ~1.43 mg/mL (~3.79 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.51 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 (5.51 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 (5.51 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 | 2.6502 mL | 13.2510 mL | 26.5020 mL | |
| 5 mM | 0.5300 mL | 2.6502 mL | 5.3004 mL | |
| 10 mM | 0.2650 mL | 1.3251 mL | 2.6502 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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