2. Cell Cycle/DNA Damage
  3. Checkpoint Kinase (Chk)
  4. Chk1-IN-6

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.

Chk1-IN-6

Chk1-IN-6 Chemical Structure

CAS No. : 2428423-77-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Chk1-IN-6 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Chk1

16.1 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MV4-11 IC50
0.14 μM
Compound: 6c
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
[PMID: 34665631]
Z-138 IC50
3.28 μM
Compound: 6c
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
[PMID: 34665631]
In Vitro

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.

Chk1-IN-6 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0, 50, 100, 200, 400 and 800 nM
Incubation Time: 2 h
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.
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 20 mg/kg p.o. T1/2 10.84 h
Mice 20 mg/kg p.o. Tmax 4.00 h
Mice 20 mg/kg p.o. Cmax 1447 ng/mL
Mice 20 mg/kg p.o. AUC0-t 17679 ng·h/mL
Mice 20 mg/kg p.o. AUC0-∞ 22679 ng·h/mL
Mice 20 mg/kg p.o. MRT0-∞ 14.73 h
In Vivo

k1-IN-6 (Compound 6c) (5-30 mg/kg, p.o., once daily for 21 days) significantly inhibits tumor growth in vivo in a dose-dependent manner in the MV-4-11 xenograft mouse model[1].
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.

Animal Model: MV-4-11 xenograft model established in NU/NU nude mice[1]
Dosage: 5, 15 and 30 mg/kg
Administration: Oral administration (p.o.), once daily for 21 days
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.
Animal Model: HT-29 xenograft model established in NU/NU nude mice[1]
Dosage: 30 mg/kg with or without Gemcitabine
Administration: Oral administration (p.o.), continuously for 5 days/week for 22 days
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%).
Molecular Weight

365.36

Formula

C16H18F3N7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC(C=C1)=NC=C1NC2=NC=C(C(F)(F)F)C(NCCC(C)(C)N)=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7370 mL 13.6851 mL 27.3703 mL
5 mM 0.5474 mL 2.7370 mL 5.4741 mL
View the 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.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
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
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Chk1-IN-6 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Chk1-IN-62428423-77-0Checkpoint Kinase (Chk)Checkpoint kinase 1MV-4-11 cellsHT-29 cellsmice modelorally bioavailableInhibitorinhibitorinhibit

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