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Merck

SML3054

Sigma-Aldrich

CHIR124

≥98% (HPLC)

别名:

4-[((3S)-1-Azabicyclo[2.2.2]oct-3-yl)amino]-3-(1H-benzimidazol-2-yl)-6-chloroquinolin-2(1H)-one, 4-[(3S)-1-Azabicyclo[2.2.2]oct-3-ylamino]-3-(1H-benzimidazol-2-yl)-6-chloro-2(1H)-quinolinone, CHIR 124, CHIR-124, f 4-[((3S)-
quinuclidin-3-yl)amino]-3-benzimidazol-2-yl-6-chloro-hydroquinolin-2- one

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About This Item

经验公式(希尔记法):
C23H22ClN5O
分子量:
419.91
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

O=C1NC2=CC=C(Cl)C=C2C(N[C@@H]3CN4CCC3CC4)=C1C5=NC6=C(C=CC=C6)N5

InChI

1S/C23H22ClN5O/c24-14-5-6-16-15(11-14)21(25-19-12-29-9-7-13(19)8-10-29)20(23(30)28-16)22-26-17-3-1-2-4-18(17)27-22/h1-6,11,13,19H,7-10,12H2,(H,26,27)(H2,25,28,30)/t19-/m1/s1

InChI 密鑰

MOVBBVMDHIRCTG-LJQANCHMSA-N

生化/生理作用

CHIR124 is a potent and selective inhibitor of checkpoint kinase 1 (Chk1)( IC50 = 0.3 nM) that produces G2-M abrogation which induces chemosensitisation. It also inhibits PDGFR and FLT3 (IC50 = 6.6 nM and 5.8 nM respectively). CHIR-124 inhibits Pgp activity in multidrug-resistant cell lines KB-V1 and A2780-Pac-Res.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Rida Zahra et al.
PloS one, 15(6), e0233993-e0233993 (2020-06-03)
Multidrug resistance (MDR) to chemotherapeutic drugs remains one of the major impediments to the treatment of cancer. Discovery and development of drugs that can prevent and reverse the acquisition of multidrug resistance constitute a foremost challenge in cancer therapeutics. In
Archie N Tse et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 13(2 Pt 1), 591-602 (2007-01-27)
Chk1 kinase is a critical regulator of both S and G(2)-M phase cell cycle checkpoints in response to DNA damage. This study aimed to evaluate the biochemical, cellular, and antitumor effects of a novel Chk1 inhibitor, CHIR124. CHIR-124 was evaluated

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