| Identification | Back Directory | [Name]
CHIR-124 | [CAS]
405168-58-3 | [Synonyms]
CS-2141
CHIR-124
CHIR-124
(CHIR124
CHIR-124 USP/EP/BP
2(1H)-Quinolinone, 4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylaMino]-3-(1H-benziMidazol-2-yl)-6-chloro-
4-[((3S)-1-Azabicyclo[2.2.2]oct-3-yl)amino]-3-(1H-benzimidazol-2-yl)-6-chloroquinolin-2(1H)-one | [Molecular Formula]
C23H22ClN5O | [MDL Number]
MFCD14636453 | [MOL File]
405168-58-3.mol | [Molecular Weight]
419.91 |
| Chemical Properties | Back Directory | [density ]
1.46 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥10.5 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming | [form ]
solid | [pka]
9.00±0.70(Predicted) | [color ]
Light yellow to brown | [InChIKey]
MOVBBVMDHIRCTG-LJQANCHMSA-N | [SMILES]
N1C2=C(C=C(Cl)C=C2)C(N[C@H]2C3CCN(CC3)C2)=C(C2NC3=CC=CC=C3N=2)C1=O |
| Hazard Information | Back Directory | [Description]
Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. CHIR124 is a cell-permeable, quinolone-based inhibitor of Chk1 (IC50 = 0.3 nM in vitro). It demonstrates high selectivity for Chk1 by displaying inhibitory values 2,000-fold higher against Chk2 (IC50 = 0.7 μM). In synergy with topoisomerase I poisons or ionizing radiation, CHIR124 can inhibit the growth of p53-mutant solid tumor cells both in vitro and in a xenograft model, potentiating tumor apoptosis. | [Uses]
CHIR 124 is a cell-permeable molecule with a quinolone-based structure. It inhibits checkpoint kinase 1 (Chk1) which regulates S and G2-M cekk cycle checkpoints in response to DNA damage. Application towards inhibition of tumor cell growth. | [in vivo]
CHIR-124 (10 or 20 mg/kg, p.o.) does not have a significant effect on tumor growth when compared with the vehicle-treated group, but it potentiates the growth inhibitory effect of CPT-11 in a human breast carcinoma xenograft model. The potentiation of the tumor growth inhibitory effect of CPT-11 by CHIR-124 is associated with an increase in apoptosis induction in the tumors. CHIR-124 reverses the suppression of phospho-H3 staining induced by CPT-11, indicating abrogation of the G2-M checkpoint by CHIR-124[1]. | [IC 50]
Chk1: 0.3 nM (IC50); Chk2: 697.4 nM (IC50); PDGFR: 6.6 nM (IC50); FLT3: 5.8 nM (IC50); Cdk4/cyclin D: 2.05 μM (IC50); CDC2/cyclin B: 0.5057 μM (IC50); Cdk2/cyclin A: 0.1911 μM (IC50); bFGFR: 2.01 μM (IC50); FGFR3: 1.29 μM (IC50); VEGFR2 FLK1: 0.5779 μM (IC50); VEGFR1 FLT1: 0.4636 μM (IC50); PKCα: 0.58 μM (IC50); PKAβ I: 2.25 μM (IC50); PKCβ II: 0.58 μM (IC50); PKCγ: 0.11 μM (IC50); ERK2: 4.31 μM (IC50); PKA: 0.1031 μM (IC50); GSK3: 0.0233 μM (IC50) | [storage]
Store at -20°C | [References]
[1]. tse an, rendahl kg, sheikh t, et al. chir-124, a novel potent inhibitor of chk1, potentiates the cytotoxicity of topoisomerase i poisons in vitro and in vivo. clinical cancer research, 2007, 13(2): 591-602.
[2]. tao yg, leteur c, yang cy, et al. radiosensitization by chir-124, a selective chk1 inhibitor effects of p53 and cell cycle checkpoints. cell cycle, 2007, 8(8): 1196-1205. |
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BOC Sciences
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1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
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www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
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