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CCT020312 (CCT-020312) is a novel and potent EIF2AK3 activator that sensitizes cancer cells with defective taxane-induced EIF2A phosphorylation to paclitaxel treatment.
| Targets |
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| ln Vitro |
Upon subjecting HT29 cells to CCT020312 for a whole day, a concentration-dependent decrease in P-S608-pRB signal was observed, exhibiting a linear response ranging from 1.8 to 6.1 μM [1]. Even while CCT020312 treatment only lasted for two hours and the substance was later removed, it successfully suppressed cell proliferation (measured at 96 hours), suggesting that CCT020312 is capable of eliciting long-lasting rather than temporary cellular inhibition [1]. After subjecting HT29 cells to a 24-hour treatment of 10 μM CCT020312, the amount of G1/S cyclins D1, D2, E, and A as well as the CDK catalytic subunit CDK2 were reduced. Conversely, the levels of the CDK inhibitor p27KIP1 were elevated in these cells [1].
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| ln Vivo |
Upon administering the PERK activator CCT020312 (1–5 mg/kg; intraperitoneally; once daily for three days) to 15-week-old wild-type mice, brain homogenates demonstrated elevated levels of phosphorylated PERK and NRF2 [2]. In the Morris water maze, P301S transgenic mice given CCT020312 (2 mg/kg; i.p.; once daily for 6 weeks) fared far better [2].
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| Animal Protocol |
Animal/Disease Models: 9weeks old P301S tau transgenic mice[2]
Doses: 2 mg/kg Route of Administration: intraperitoneal (ip)injection; one time/day for 6 weeks Experimental Results: P301S transgenic mice treated with CCT020312 performed Dramatically better in Morris water maze. |
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| References |
| Molecular Formula |
C31H30BR2N4O2
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|---|---|
| Molecular Weight |
650.403505802155
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| Exact Mass |
648.073
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| CAS # |
324759-76-4
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| PubChem CID |
3108148
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
39
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| Complexity |
950
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1C=CC(=CC=1)C1CC(C2C(NC3C=CC(=CC=3C=2C2C=CC=CC=2)Br)=O)=NN1C(CCN(CC)CC)=O
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| InChi Key |
OAXDKXMGESZLKV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H30Br2N4O2/c1-3-36(4-2)17-16-28(38)37-27(20-10-12-22(32)13-11-20)19-26(35-37)30-29(21-8-6-5-7-9-21)24-18-23(33)14-15-25(24)34-31(30)39/h5-15,18,27H,3-4,16-17,19H2,1-2H3,(H,34,39)
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| Chemical Name |
6-bromo-3-[3-(4-bromophenyl)-2-[3-(diethylamino)propanoyl]-3,4-dihydropyrazol-5-yl]-4-phenyl-1H-quinolin-2-one
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| Synonyms |
CCT 020312 CCT-020312 CCT020312
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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 : ~100 mg/mL (~153.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.20 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 (3.20 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 (3.20 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 | 1.5375 mL | 7.6876 mL | 15.3752 mL | |
| 5 mM | 0.3075 mL | 1.5375 mL | 3.0750 mL | |
| 10 mM | 0.1538 mL | 0.7688 mL | 1.5375 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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