| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
| Targets |
CLK2 (IC50 = 0.006 μM)
|
|---|---|
| ln Vitro |
CC-671 (compound 23) is a dual inhibitor of TTK protein kinase and CDC2-like kinase (CLK2), with IC50 values for TTK and CLK2 of 0.005 and 0.006 μM, respectively. Only four kinases—CLK2, CAMKK2, PIP4K22, and JNK—show cellular binding of 75% or more in HCT-116 cell lysates treated with CC-671 at 3 μM for 1 hour[1].
|
| ln Vivo |
CC-671 (compound 23) exhibits a noteworthy 71% tumor growth inhibition (TGI) (vehicle-treated/vehicle) ×100%) at doses of 10 and 20 mg/kg when administered on a once-every-three-day (q3d) basis. Body weight loss (BWL) was greater in the group treated with CC-671 (20 mg/kg) than in the group treated with 10 mg/kg (17% vs. 5%)[1].
|
| Enzyme Assay |
Compound 23 (CC-671) kinase selectivity profile is evaluated. The CC-671 concentration is maintained at 3 μM throughout the screen. Kinase binding assays are used to quantify the TTK binding affinity. The ATP-competitive kinase inhibitor scaffold, which is proprietary and labeled with Alexa Fluor 647, is the basis for the kinase binding assays[1].
|
| Animal Protocol |
Subcutaneous injection of 5×106 Cal-51 cells is administered to female SCID mice. Randomized mice bearing 125 mm3 tumors are administered CC-671 (compound 23) intravenously at different intervals and doses (n=8–10/group). For the course of the investigation, tumors are measured twice a week. Tumor volumes are computed by measuring each tumor's long and short axes in millimeters with a digital caliper[1].
|
| References |
| Molecular Formula |
C28H28N6O4
|
|---|---|
| Molecular Weight |
512.57
|
| Exact Mass |
512.2172
|
| Elemental Analysis |
C, 65.61; H, 5.51; N, 16.40; O, 12.49
|
| CAS # |
1618658-88-0
|
| Related CAS # |
1618658-88-0
|
| Appearance |
Solid powder
|
| SMILES |
CC1=NC2=C(O1)C=C(C=C2)C3=CNC4=C3C(=NC(=N4)NC5=C(C=C(C=C5)C(=O)NC)OC)OC6CCCC6
|
| InChi Key |
CWJLAVRXVFHDSJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C28H28N6O4/c1-15-31-21-10-8-16(12-23(21)37-15)19-14-30-25-24(19)27(38-18-6-4-5-7-18)34-28(33-25)32-20-11-9-17(26(35)29-2)13-22(20)36-3/h8-14,18H,4-7H2,1-3H3,(H,29,35)(H2,30,32,33,34)
|
| Chemical Name |
4-[[4-cyclopentyloxy-5-(2-methyl-1,3-benzoxazol-6-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxy-N-methylbenzamide
|
| Synonyms |
CC671; CC 671; CC-671
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ≥ 60 mg/mL (~117.1 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.06 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 (4.06 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (4.06 mM) 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 | 1.9510 mL | 9.7548 mL | 19.5095 mL | |
| 5 mM | 0.3902 mL | 1.9510 mL | 3.9019 mL | |
| 10 mM | 0.1951 mL | 0.9755 mL | 1.9510 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA