| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
In ES cells, CKI-7 treatment (0.1-10 μM; 5 days) dramatically enhanced the number of cells positive for the neural markers βIII-tubulin and nestin, as well as the expression of the early neuroectoderm marker Sox1 in a concentration-dependent manner [1]. Day 5 β-catenin stabilization induced by SFEB was decreased by CKI-7 (5 μM; 5 days; ES cells) treatment, suggesting that CKI-7 suppresses Wnt signaling [1].
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| ln Vivo |
Using a newly isolated Philadelphia chromosome-positive acute lymphoblastic leukemia cell line, the in vivo dose-dependent anticancer efficacy of CKI-7 was established in a SCID-Beige mouse systemic tumor model. The activation of caspase 3 and subsequent cell cycle-dependent death are confirmed by standard cell cycle synchronization tests upon exposure to CKI-7 [2].
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| Cell Assay |
RT-PCR[1]
Cell Types: Mouse ES cells Tested Concentrations: 0.1-10 μM Incubation Duration: 5 days Experimental Results: The expression of early neuroectoderm marker Sox1 was Dramatically increased, and the neural markers nestin and βIII-tubulin were Dramatically increased. The number of positive cells increased Dramatically in a concentration-dependent manner. Western Blot Analysis[1] Cell Types: Mouse ES cells Tested Concentrations: 5 μM Incubation Duration: 5 days Experimental Results: Inhibition of SFEB-induced β-catenin stabilization on day 5. |
| References |
[1]. Osakada F, et al. In vitro differentiation of retinal cells from human pluripotent stem cells by small-molecule induction. J Cell Sci. 2009 Sep 1;122(Pt 17):3169-79.
[2]. Mark G. Frattini, et al. Small Molecule Inhibition of Cdc7, a Key Cell Cycle Regulator and Novel Therapeutic Target, Successfully Inhibits Leukemia Cell Growth in Vitro and in Vivo. Blood (2008) 112 (11): 2668. [3]. Chijiwa T, et al. A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis. J Biol Chem. 1989 Mar 25;264(9):4924-7. [4]. Rena G, et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 2004 Jan;5(1):60-5. |
| Molecular Formula |
C₁₁H₁₂CLN₃O₂S
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|---|---|
| Molecular Weight |
285.75
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| CAS # |
120615-25-0
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| Related CAS # |
CKI-7;1177141-67-1
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
NCCNS(C1=C2C(C=CN=C2)=C(Cl)C=C1)(=O)=O
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| Synonyms |
CKI7 free base; CKI 7 free base
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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 : ~25 mg/mL (~87.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.28 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 (7.28 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 (7.28 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 | 3.4996 mL | 17.4978 mL | 34.9956 mL | |
| 5 mM | 0.6999 mL | 3.4996 mL | 6.9991 mL | |
| 10 mM | 0.3500 mL | 1.7498 mL | 3.4996 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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