CHIR-124 manufacturers
- CHIR-124
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- $35.00
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2026-07-27
- CAS:405168-58-3
- Purity: 98.74%
- Supply Ability: 10g
- CHIR-124
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- $3.00
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2020-02-21
- CAS:405168-58-3
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 200KG
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| | CHIR-124 Basic information |
| Product Name: | CHIR-124 | | Synonyms: | CS-2141;CHIR-124
(CHIR124;CHIR-124;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;CHIR-124 USP/EP/BP;Platelet-derived growth factor receptor,PDGFR,CHIR-124,Checkpoint Kinase (Chk),CD135,Fms like tyrosine kinase 3,Cluster of differentiation antigen 135,inhibit,Apoptosis,Inhibitor,FLT3;(S)-3-(1H-Benzo[d]imidazol-2-yl)-6-chloro-4-(quinuclidin-3-ylamino)quinolin-2(1H)-one , CHIR-124 | | CAS: | 405168-58-3 | | MF: | C23H22ClN5O | | MW: | 419.91 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 405168-58-3.mol |  |
| | CHIR-124 Chemical Properties |
| 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 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | CHIR-124 Usage And Synthesis |
| 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) | | 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. |
| | CHIR-124 Preparation Products And Raw materials |
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