Chk1-IN-6
Based on 1 Customer Validation
Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC50 of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma.
For research use only. We do not sell to patients.
- Purity: 98.39%
- CAS No.: 2428423-77-0
- Formula: C16H18F3N7
- Molecular Weight:365.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Chk1 16.1 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
0.14 μM
Compound: 6c
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Antiproliferation activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Antiproliferation activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
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[PMID: 34665631] |
| Z-138 | IC50 |
3.28 μM
Compound: 6c
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Antiproliferation activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Antiproliferation activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
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[PMID: 34665631] |
Chk1-IN-6 (Compound 6c) shows antiproliferative activity of MV-4-11 and Z138 cells with IC50 values of 0.14 and 3.28 μM[1].
Chk1-IN-6 (0-5 nM, 72 h) combined with Gemcitabine shows a synergistic effect on HT-29, A549, and RPMI-8226[1].
Chk1-IN-6 (0-800 nM, 2 h) inhibits the phosphorylated S296 CHK1 (pS296 CHK1) and induces the phosphorylated S345 CHK1 (pS345 CHK1) in MV-4-11[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 cells
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Concentration:0, 50, 100, 200, 400 and 800 nM
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Incubation Time:2 h
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Result:Caused a dose-dependent decrease in pS296 CHK1.
Induced a dose-dependent increase in pS345.
With Gemcitabine at 1.1 μM in different concentrations could lead to a pronounced reduction in pS296 CHK1 and induced an increase in γ-H2A.X.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 20 mg/kg | p.o. | 10.84 h | 4.00 h | 1447 ng/mL | 17679 ng·h/mL | 22679 ng·h/mL | 14.73 h |
Chk1-IN-6 (5-30 mg/kg, p.o., continuously for 5 days/week for 22 days) shows synergistic anticancer effect of with Gemcitabine in the HT-29 xenograft mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV-4-11 xenograft model established in NU/NU nude mice[1]
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Dosage:5, 15 and 30 mg/kg
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Administration:Oral administration (p.o.), once daily for 21 days
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Result:Significantly inhibited tumor growth in vivo in a dose-dependent manner and showed inhibition of tumor growth of 51.62, 95.52, and 94.90% at doses of 5, 15, 30 mg/kg, respectively.
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Animal Model:HT-29 xenograft model established in NU/NU nude mice[1]
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Dosage:30 mg/kg with or without Gemcitabine
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Administration:Oral administration (p.o.), continuously for 5 days/week for 22 days
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Result:Showed mild antitumor effect with T/C values of 69.05% and in combination with Gemcitabine showed a significant increase in efficacy (T/C = 11.99%).
Chemical Information
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CAS No. 2428423-77-0
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Appearance Solid
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Molecular Weight 365.36
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Formula C16H18F3N7
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Color White to off-white
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SMILES
N#CC(C=C1)=NC=C1NC2=NC=C(C(F)(F)F)C(NCCC(C)(C)N)=N2
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (68.43 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.7370 mL | 13.6851 mL | 27.3703 mL | 68.4257 mL |
| 5 mM | 0.5474 mL | 2.7370 mL | 5.4741 mL | 13.6851 mL | |
| 10 mM | 0.2737 mL | 1.3685 mL | 2.7370 mL | 6.8426 mL | |
| 15 mM | 0.1825 mL | 0.9123 mL | 1.8247 mL | 4.5617 mL | |
| 20 mM | 0.1369 mL | 0.6843 mL | 1.3685 mL | 3.4213 mL | |
| 25 mM | 0.1095 mL | 0.5474 mL | 1.0948 mL | 2.7370 mL | |
| 30 mM | 0.0912 mL | 0.4562 mL | 0.9123 mL | 2.2809 mL | |
| 40 mM | 0.0684 mL | 0.3421 mL | 0.6843 mL | 1.7106 mL | |
| 50 mM | 0.0547 mL | 0.2737 mL | 0.5474 mL | 1.3685 mL | |
| 60 mM | 0.0456 mL | 0.2281 mL | 0.4562 mL | 1.1404 mL |
Chk1-IN-6 Related Classifications
HY-139901 Related Classifications
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