| Size | Price | Stock | Qty |
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| 5mg |
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| 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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| ln Vitro |
The IC50 values of IC261 for Ckiδ, Ckiε, and Ckiα1 are 1 μM, 1 μM, and 16 μM, respectively. It is a selective ATP-competitive CK1 inhibitor. With an IC50 > 100 μM, IC261 exhibits minimal action against PKA, p34cdc2, and p55fyn [1]. In AC1-M88 cells, IC261 causes centrosome amplification, spindle abnormalities, and mitotic arrest. After 12 hours, IC261 (1 μM) increases G2/M cells, and 24 hours later, it promotes cell death in AC1-M88. Extravillous trophoblast hybrid cells undergo apoptosis in response to IC261 (1 μM) as well [2]. Numerous pancreatic tumor cell lines, such as ASPC-1, BxPc3, Capan-1, Colo357, MiaPaCa-2, Panc1, Panc89, PancTu-1, and PancTu-2 cells, are inhibited in their ability to proliferate by IC261 (1.25 μM). Pancreatic tumor cells' CD95-mediated apoptosis is specifically enhanced by IC261 (1.25 μM) [3].
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| ln Vivo |
In SCID mice, IC261 (20.5 mg/kg) suppresses the formation of PancTu-2 cell tumors, downregulates several anti-apoptotic proteins, including CK1δ/∊, KRAS, and IL6, and increases the expression of p21, ATM, CHEK1, and STAT1 [3].
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| References |
[1]. Mashhoon N, et al. Crystal structure of a conformation-selective casein kinase-1 inhibitor. J Biol Chem. 2000 Jun 30;275(26):20052-60.
[2]. Stöter M, et al. Inhibition of casein kinase I delta alters mitotic spindle formation and induces apoptosis in trophoblast cells. Oncogene. 2005 Dec 1;24(54):7964-75. [3]. Brockschmidt C, et al. Anti-apoptotic and growth-stimulatory functions of CK1 delta and epsilon in ductal adenocarcinoma of the pancreas are inhibited by IC261 in vitro and in vivo. Gut. 2008 Jun;57(6):799-80 |
| Molecular Formula |
C18H17NO4
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|---|---|
| Molecular Weight |
311.3319
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| CAS # |
186611-52-9
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| SMILES |
O(C([H])([H])[H])C1C([H])=C(C([H])=C(C=1/C(/[H])=C1/C(N([H])C2=C([H])C([H])=C([H])C([H])=C/12)=O)OC([H])([H])[H])OC([H])([H])[H]
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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 : ≥ 33 mg/mL (~106.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2120 mL | 16.0601 mL | 32.1203 mL | |
| 5 mM | 0.6424 mL | 3.2120 mL | 6.4241 mL | |
| 10 mM | 0.3212 mL | 1.6060 mL | 3.2120 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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