1200126-26-6

1200126-26-6 structure

Name: GNE-900
Chemical Name: 3-[4-(Piperidin-1-Ylmethyl)phenyl]-9h-Pyrrolo[2,3-B:5,4-C']dipyridine-6-Carbonitrile
CAS Number: 1200126-26-6
Molecular Formula: C₂₃H₂₁N₅
Molecular Weight: 367.446
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2018-07-03 09:05:25
Modify Date: 2025-08-25 05:45:10
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity[1].

Name	3-[4-(Piperidin-1-Ylmethyl)phenyl]-9h-Pyrrolo[2,3-B:5,4-C']dipyridine-6-Carbonitrile
Synonyms	3-[4-(Piperidin-1-Ylmethyl)phenyl]-9h-Pyrrolo[2,3-B:5,4-C']dipyridine-6-Carbonitrile 9H-Pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile, 3-[4-(1-piperidinylmethyl)phenyl]- 3-[4-(1-Piperidinylmethyl)phenyl]-9H-pyrido[4',3':4,5]pyrrolo[2,3-b]pyridine-6-carbonitrile GNE-900

Description	GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity[1].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> Checkpoint Kinase (Chk)
Target	Chk1:0.0011 μM (IC50) Chk2:1.5 μM (IC50)
In Vitro	GNE-900 (1 µM; 1-48 h) 在 HT-29 细胞中与吉西他滨 (50 nM) 联合使用时，可诱导细胞凋亡并增加裂解的 PARP 的表达[1]。 Apoptosis Analysis[1] Cell Line: HT-29 cells Concentration: 1 µM Incubation Time: 1-48 h Result: Inducesd apoptosis with increased the expression of cleaved PARP when combination with gemcitabine (50 nM).
In Vivo	GNE-900 (2.5-40 mg/kg; p.o.; once) 与gemcitabine (HY-17026) 联用能降低肿瘤体积并增加 DNA 损伤和 γ-H2AX 的表达水平在大鼠中[1]。 Animal Model: Sprague-Dawley rats (HT-29 tumor xenografts)[1] Dosage: 2.5-40 mg/kg (received a dose of gemcitabine 120 mg/kg) Administration: P.o.; once Result: Decreased the tumor volume and resulted in significant enhancement of DNA damage, increased γ-H2AX levels.
References	[1]. Blackwood E, et al. Combination drug scheduling defines a "window of opportunity" for chemopotentiation of gemcitabine by an orally bioavailable, selective ChK1 inhibitor, GNE-900. Mol Cancer Ther. 2013 Oct;12(10):1968-80.

Density	1.3±0.1 g/cm3
Boiling Point	633.4±55.0 °C at 760 mmHg
Molecular Formula	C₂₃H₂₁N₅
Molecular Weight	367.446
Flash Point	336.9±31.5 °C
Exact Mass	367.179688
LogP	4.44
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.727

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