CCT245737
Based on 4 publication(s) in Google Scholar
CCT245737 (SRA737) is an orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM.
For research use only. We do not sell to patients.
- Purity: 99.48%
- CAS No.: 1489389-18-5
- Formula: C16H16F3N7O
- Molecular Weight:379.34
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) CCT245737
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IF
Biological Activity
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Chk1 1.3 nM (IC50) |
Chk2 2440 nM (IC50) |
ERK8 130 nM (IC50) |
PKD1 298 nM (IC50) |
RSK2 361 nM (IC50) |
RSK1 362 nM (IC50) |
FLT3 582 nM (IC50) |
MARK3 698 nM (IC50) |
NUAK1 711 nM (IC50) |
CLK2 1370 nM (IC50) |
BRSK1 1660 nM (IC50) |
AMPK 2970 nM (IC50) |
PHK 3470 nM (IC50) |
CDK2/CyclA 3850 nM (IC50) |
CDK1/CyclB 9030 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
>10000 nM
Compound: CCT245737
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Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
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[PMID: 38547734] |
| A549 | IC50 |
>10000 nM
Compound: CCT245737
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Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
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[PMID: 38547734] |
| Calu-6 | GI50 |
0.046 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay
Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay
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[PMID: 26295308] |
| Calu-6 | GI50 |
0.32 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay
Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay
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[PMID: 26295308] |
| Calu-6 | GI50 |
0.41 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs by SRB assay
Cytotoxicity against human Calu-6 cells assessed as growth inhibition measured after 96 hrs by SRB assay
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[PMID: 26295308] |
| HCT-116 | IC50 |
>10000 nM
Compound: CCT245737
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
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[PMID: 38547734] |
| HEK293 | GI50 |
1.387 μM
Compound: CCT245737
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Antiproliferative activity against human HEK293 cells after 72 hrs by MTS assay
Antiproliferative activity against human HEK293 cells after 72 hrs by MTS assay
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[PMID: 29684894] |
| HL-60 | IC50 |
>10000 nM
Compound: CCT245737
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Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
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[PMID: 38547734] |
| HT-29 | GI50 |
0.09 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay
Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay
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[PMID: 26295308] |
| HT-29 | GI50 |
0.39 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay
Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay
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[PMID: 26295308] |
| HT-29 | GI50 |
0.7 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs by SRB assay
Cytotoxicity against human HT-29 cells assessed as growth inhibition measured after 96 hrs by SRB assay
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[PMID: 26295308] |
| HT-29 | GI50 |
9.223 μM
Compound: CCT245737
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Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTS assay
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[PMID: 29684894] |
| HT-29 | IC50 |
>10000 nM
Compound: CCT245737
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Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
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[PMID: 38547734] |
| HT-29 | IC50 |
176.62 nM
Compound: CCT245737
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Synergistic antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs in presence of 50 nM gemcitabine by CCK-8 assay
Synergistic antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs in presence of 50 nM gemcitabine by CCK-8 assay
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[PMID: 38547734] |
| MDA-MB-468 | IC50 |
>10000 nM
Compound: CCT245737
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Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
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[PMID: 38547734] |
| MIA PaCa-2 | GI50 |
0.066 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay
Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay
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[PMID: 26295308] |
| MIA PaCa-2 | GI50 |
0.43 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay
Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay
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[PMID: 26295308] |
| MIA PaCa-2 | GI50 |
1.3 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs by SRB assay
Cytotoxicity against human MIA PaCa-2 cells assessed as growth inhibition measured after 96 hrs by SRB assay
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[PMID: 26295308] |
| MV4-11 | IC50 |
244.6 nM
Compound: CCI245737
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Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
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[PMID: 37584545] |
| MV4-11 | IC50 |
211.13 nM
Compound: CCT-245737
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Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader
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[PMID: 38389894] |
| OVCAR-3 | IC50 |
>10000 nM
Compound: CCT245737
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Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by by CCK-8 assay
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[PMID: 38547734] |
| SW-620 | GI50 |
0.33 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay
Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs in presence of Gemcitabine by SRB assay
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[PMID: 26295308] |
| SW-620 | GI50 |
1.8 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay
Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs in presence of SN38 by SRB assay
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[PMID: 26295308] |
| SW-620 | GI50 |
5.4 μM
Compound: Chemical probe: CCT245737
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Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs by SRB assay
Cytotoxicity against human SW620 cells assessed as growth inhibition measured after 96 hrs by SRB assay
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[PMID: 26295308] |
CCT245737 (10 μM) shows >80% inhibition of a panel of 124 kinases, including ERK8, PKD1, RSK2 and RSK1 with IC50s of 130, 298, 361 and 362 nM[1]. CCT245737 abrogates an VP-16-induced G2 checkpoint in HT29, SW620, MiaPaCa-2, and Calu6 cell lines, with IC50s ranging from 30 to 220 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1489389-18-5
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Appearance Solid
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Molecular Weight 379.34
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Formula C16H16F3N7O
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Color White to yellow
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SMILES
FC(F)(F)C(C=NC(NC1=CN=C(C#N)C=N1)=C2)=C2NC[C@H]3CNCCO3
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Synonyms
SRA737
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Pancancer Fine-Mapping of Mutational Intolerance Identifies CHEK1 as an Immunosuppressive Driver in Lung Adenocarcinoma. [Abstract]2026 May;13(25):e21265. PMID: 41722056 -
Nucleic Acids Res
BTG3-dependent VCP/p97 nuclear translocation is required for efficient repair of UV-induced DNA lesions. [Abstract]2025 Jul 8;53(13):gkaf626. PMID: 40626560
CCT245737 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2025 Jul 8;53(13):gkaf626. [Abstract]
XPC K63-linked ubiquitylation was enhanced by CHK1 inhibition. 293T cells were pretreated with 5 μM CHK1 inhibitor CCT245737 (CHK1i) for 2 h before UV, and XPC K63-ubiquitin modification was analyzed.
CCT245737 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2025 Jul 8;53(13):gkaf626. [Abstract]
CHK1 inhibition recapitulated the effect of BTG3 KO in delaying VCP/p97 nuclear translocation. Confocal microscopic imaging of VCP/p97 was conducted with HaCaT cells pretreated or not with CHK1i for 2 h.
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Solvent & Solubility
DMSO : 50 mg/mL (131.81 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cytotoxicity is determined as the drug concentration that gives 50% inhibition of tumor cell proliferation (GI50) using a 96 h Sulforhodamine B (SRB) assay. Inhibition of intracellular CHK1 activity is measured using a cell based ELISA for the abrogation of an VP-16 induced G2 checkpoint (mitosis induction assay, MIA). The IC50 for G2 checkpoint abrogation (MIA) is determined in the presence of nocodazole using UCN01 as a positive control. The activity index (AI) is used as a measure of the compounds ability to induce mitosis relative to its toxicity (i.e., ratio of MIA IC50: 96 h SRB GI50). Routine potentiation studies are carried out using a fixed concentration (GI50) of either LY 188011 or SN38 in combination with a range of CCT245737 concentrations to determine the combination GI50 of CCT245737. The ability of CCT245737 to enhance LY 188011 or SN38 cell killing is expressed as a potentiation index (PI) equal to the ratio of the GI50 for CCT245737 alone versus the combination GI50 for CCT245737. PI values > 1 indicate potentiation of the genotoxic activity. In addition, a series of experiments is carried out using fixed, non- or minimally toxic concentrations of CCT245737 (≤GI20) with a range of different concentrations of LY 188011 or SN38 to determine the extent to which CCT245737 enhances drug cytotoxicity compared with the genotoxic agent alone, i.e. conventional PI (ratio GI50 genotoxic alone: GI50 genotoxic combined with non-toxic CCT245737 concentration, Con PI)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Human HT29 colorectal carcinoma cells are injected s.c into the flanks of female NCr athymic mice 6-8 weeks of age. Dosing commenced 5 days after transplantation when tumors reach a mean diameter of 5.5 mm. LY 188011 (100 mg/kg i.v.) is dosed in saline on days 0, 7 and 14 and compounds 4 (CCT245737) and 41 (150 mg/kg p.o.) in 10% DMSO 20% PEG 400, 5% Tween 80, 65% water, 24 and 48 h after each dose of LY 188011. Tumors are measured and body weights recorded three times weekly. Animals are culled on an individual basis when tumors reach a predetermined humane endpoint (mean diameter <15 mm)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Osborne JD, et al. Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737). J Med Chem. 2016 Jun 9;59(11):5221-37. [Content Brief]
[2]. Walton MI, et al. The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eμ-MYC driven B-cell lymphoma. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6362 mL | 13.1808 mL | 26.3616 mL | 65.9039 mL |
| 5 mM | 0.5272 mL | 2.6362 mL | 5.2723 mL | 13.1808 mL | |
| 10 mM | 0.2636 mL | 1.3181 mL | 2.6362 mL | 6.5904 mL | |
| 15 mM | 0.1757 mL | 0.8787 mL | 1.7574 mL | 4.3936 mL | |
| 20 mM | 0.1318 mL | 0.6590 mL | 1.3181 mL | 3.2952 mL | |
| 25 mM | 0.1054 mL | 0.5272 mL | 1.0545 mL | 2.6362 mL | |
| 30 mM | 0.0879 mL | 0.4394 mL | 0.8787 mL | 2.1968 mL | |
| 40 mM | 0.0659 mL | 0.3295 mL | 0.6590 mL | 1.6476 mL | |
| 50 mM | 0.0527 mL | 0.2636 mL | 0.5272 mL | 1.3181 mL | |
| 60 mM | 0.0439 mL | 0.2197 mL | 0.4394 mL | 1.0984 mL | |
| 80 mM | 0.0330 mL | 0.1648 mL | 0.3295 mL | 0.8238 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.6590 mL |
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