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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
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 419.91
Formula C23H22ClN5O
CAS Number 405168-58-3
Purity >98%
Solubility DMSO 7 mg/mL
Storage at -20°C
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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Keywords: CHIR-124 supplier, Checkpoint, inhibitors

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