2. Cell Cycle/DNA Damage
  3. Checkpoint Kinase (Chk)
  4. CHK1-IN-9

CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026).

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CHK1-IN-9 Chemical Structure

CHK1-IN-9 Chemical Structure

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CHK1-IN-9 Related Antibodies

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Description

CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026)[1].

IC50 & Target

Chk1

0.55 nM (IC50)

In Vitro

CHK1-IN-9 (compound 11) (11.11, 33.33, 100, and 300 nM, 16 h) can inhibit the proliferation of tumor cells, with the IC50 value of 202 nM for MV-4-11 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CHK1-IN-9 Related Antibodies

Cell Proliferation Assay [1]

Cell Line: OVCAR3, HT-29, A549, HL-60, HCT116, A2780 and MDAMB-468 cells
Concentration: 11.11, 33.33, 100, and 300 nM
Incubation Time: 16 h
Result: Alone had an IC50 value of 1166.5 nM for HT-29, and 63.53 nM when combined with Gemcitabine (HY-17026).
In Vivo

CHK1-IN-9 (compound 11) (30 mg/kg/day for 21 days，iv or po) demonstrates a tumor growth inhibition (TGI) value of 20.6% in the HT-29 xenograft mouse model when used alone, and shows greater antitumor activity (TGI = 42.8%) when combined with Gemcitabine (HY-17026)[1].

Pharmacokinetic Analysis in the HT-29 xenograft mouse model Model[1]

Route Dose (mg/kg) C0 (ng/mL) Cmax (ng/mL) T1/2 (h) Tmax (h) AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) MRT0-t (h) MRT0-t (h) Cl (mL/kg/min) Vss (L/kg) F (%)
i.v. 2 860 526 5.70 0.08 327 341 2.67 3.91 98.4 23.3 /
p.o. 10 / 81.1 1.51 0.08 40.7 47.3 1.00 1.65 / / 2.77

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

412.40

Formula

C19H18F2N8O
SMILES

O=C1C=CC2=NC(NC3=CN=C(C#N)C(N[C@H]4CCNC4)=C3)=NC=C2N1CC(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CHK1-IN-9 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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-9Checkpoint Kinase (Chk)DNA damageMV-4-11 cellHT-29 xenograft mouse modelHT-29 cellcancercell proliferationInhibitorinhibitorinhibit

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