| 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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| Other Sizes |
Purity: ≥98%
| Targets |
CLK2 (IC50 = 0.006 μM)
CC-671 targets TTK protein kinase (Mps1), a key regulator of the spindle assembly checkpoint, and CDC2-like kinase (CLK2), which is involved in RNA splicing and gene expression. By inhibiting these kinases, CC-671 disrupts cell cycle progression and DNA repair. It is a dual inhibitor with IC50 values of 0.005 μM for TTK and 0.006 μM for CLK2. |
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| 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].
CC-671 is a potent dual inhibitor of TTK and CLK2 with IC50 values of 5 nM and 6 nM, respectively. It selectively inhibits the growth of Cal-51 triple negative breast cancer (TNBC) cells over BT-474 luminal breast cancer cells. It is a potent, selective inhibitor of multiple kinases. |
| 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].
Specific in vivo activity data for CC-671 is not extensively detailed in the available literature. As a research compound, its in vivo effects are primarily studied in the context of TTK and CLK2 inhibition and its impact on tumor growth, particularly in cancers with defective DNA repair pathways. Further studies are needed to fully characterize its in vivo efficacy and pharmacokinetic properties. |
| 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].
CC-671's activity as a kinase inhibitor is assessed using in vitro kinase assays. These assays measure the compound's ability to inhibit the phosphorylation activity of TTK and CLK2. IC50 values are determined from dose-response curves. Selectivity profiling against other kinases is performed to evaluate its specificity. |
| Cell Assay |
Cellular assays for CC-671 involve treating cancer cell lines with the compound and measuring cell proliferation, viability, and signaling pathway inhibition. The compound's effects on the spindle assembly checkpoint and RNA splicing are assessed. Its selective effects on TNBC cells are evaluated.
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| 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].
In vivo animal model protocols for CC-671 would involve its administration to tumor-bearing mice to evaluate its antitumor efficacy. The compound's effects on tumor growth, TTK and CLK2 activity in tumor tissues, and pharmacokinetic properties would be assessed. |
| ADME/Pharmacokinetics |
CC-671 has a molecular weight of 512.56 and a molecular formula of C28H28N6O4. It is soluble in DMSO at 20 mg/ml. Specific pharmacokinetic data is not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
The toxicological profile of CC-671 has not been extensively characterized. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development.
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| References | |
| Additional Infomation |
CC-671 (CAS# 1618658-88-0) is a research compound used to study TTK and CLK2 function in cancer. It is a dual inhibitor of TTK and CLK2 with IC50 values in the nanomolar range. It is not approved for clinical use and is supplied as a research chemical.
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| Molecular Formula |
C28H28N6O4
|
|---|---|
| Molecular Weight |
512.559725761414
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| Exact Mass |
512.217
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| Elemental Analysis |
C, 65.61; H, 5.51; N, 16.40; O, 12.49
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| CAS # |
1618658-88-0
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| Related CAS # |
1618658-88-0
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| PubChem CID |
117881270
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| Appearance |
Off-white to light green solid powder
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| LogP |
5.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
814
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CWJLAVRXVFHDSJ-UHFFFAOYSA-N
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| 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)
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| 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
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| Synonyms |
CC671; CC 671; CC-671
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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: ≥ 60 mg/mL (~117.1 mM)
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|---|---|
| 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 | 9.7550 mL | 19.5099 mL | |
| 5 mM | 0.3902 mL | 1.9510 mL | 3.9020 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.
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