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Merck
모든 사진(1)

주요 문서

SML3054

Sigma-Aldrich

CHIR124

≥98% (HPLC)

동의어(들):

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

실험식(Hill 표기법):
C23H22ClN5O
CAS Number:
Molecular Weight:
419.91
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

SMILES string

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 key

MOVBBVMDHIRCTG-LJQANCHMSA-N

생화학적/생리학적 작용

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

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
Siang-Boon Koh et al.
Cancer research, 78(11), 3054-3066 (2018-05-08)
Combination of cytotoxic therapy with emerging DNA damage response inhibitors (DDRi) has been limited by tolerability issues. However, the goal of most combination trials has been to administer DDRi with standard-of-care doses of chemotherapy. We hypothesized that mechanism-guided treatment scheduling

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