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CHIR-124

Cat. No. M2325
CHIR-124 Structure
Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 150  USD150 In stock
25mg USD 300  USD300 In stock
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Quality Control & Documentation
Biological Activity

CHIR-124 is a novel and potent chk1 inhibitor with an IC50 of 0.3 nM. CHIR-124 interacts synergistically with camptothecin in causing growth inhibition in MDA-MB-435 cells as determined by isobologram analysis. In HCT116 human colon carcinoma cells, CHIR-124 increased the effect of SN-38, an active metabolite of irinotecan, in a sequence-dependent manner, with the highest induction of mitotic catastrophe and apoptosis seen when CHIR-124 was given sequentially after SN-38 pretreatment. More importantly, the enhancement of cell death by CHIR-124 was markedly increased in isogenic p53-null and p21-null HCT116 cells.

Product Citations
Customer Product Validations & Biological Datas
Source Proc Natl Acad Sci U S A (2011). Figure 2. CHIR-124
Method Cell viability assay
Cell Lines A549 cells
Concentrations 1 μM
Incubation Time 72 h
Results AZD7762 and CHIR-124 increased HDACi-induced cell death of A549 but not LNCaP
Chemical Information
Molecular Weight 419.91
Formula C23H22ClN5O
CAS Number 405168-58-3
Solubility (25°C) DMSO 7 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Xiaoxue Song, et al. Synergistic targeting of CHK1 and mTOR in MYC-driven tumors

[2] Rida Zahra, et al. A cell-based high-throughput screen identifies inhibitors that overcome P-glycoprotein (Pgp)-mediated multidrug resistance

[3] Edyta Biskup, et al. Small-molecule inhibitors of Ataxia Telangiectasia and Rad3 related kinase (ATR) sensitize lymphoma cells to UVA radiation

[4] Yungan Tao, et al. Radiosensitization by Chir-124, a selective CHK1 inhibitor: effects of p53 and cell cycle checkpoints

[5] Archie N Tse, et al. CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo

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