Shanghai Nianxing Industrial Co., Ltd
China
Product Name: SKLB 1028
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Purity: 98.0%
Stocking Period: 10 Day
Contact: Yang

1350544-93-2

1350544-93-2 structure

Name: Ruserontinib
Chemical Name: 9-Isopropyl-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-(3-pyridinyl)-9H-purine-2,8-diamine
CAS Number: 1350544-93-2
Molecular Formula: C₂₄H₂₉N₉
Molecular Weight: 443.55
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2018-07-21 17:26:39
Modify Date: 2024-01-05 07:32:19
Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity[1].

Name	9-Isopropyl-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-(3-pyridinyl)-9H-purine-2,8-diamine
Synonyms	9H-Purine-2,8-diamine, 9-(1-methylethyl)-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-3-pyridinyl- 9-Isopropyl-N2-[4-(4-methyl-1-piperazinyl)phenyl]-N8-(3-pyridinyl)-9H-purine-2,8-diamine MFCD30471083

Description	Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC50 value of 55 nM for human FLT3, and has antitumor activity[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3
In Vitro	Ruserontinib (SKLB1028)可以显著抑制表达 FLT3-ITD的 mf4 -11 细胞的生长，IC50值为 0.002 μM，抑制表达 wt-FLT3 的 RS4-11 细胞增殖的 IC50值为 0.790 μM，抑制稳定表达人 FLT3ITD 的 Ba/F3 细胞生长的IC50值为 0.01 μM，抑制表达 Bcr-Abl 突变体的 K562 细胞生长的 IC50为0.190 μM[1]。 Ruserontinib (SKLB1028) (0-100 nM, 20 h)导致 MV4-11 细胞的 pro-caspase-3水平呈剂量依赖性下降，而被切割的 caspase-3 片段水平呈剂量依赖性增加，并且可以以剂量依赖的方式抑制 STAT5 和 Erk1/2 的磷酸化[1]。
In Vivo	Ruserontinib (SKLB1028)（5-70 mg/kg，每天口服一次，18 天）在 MV4-11 和 K562 异种移植 NOD-SCID 模型中具有抗肿瘤作用[1]。 Animal Model: MV4-11 and K562 xenograft NOD-SCID models[1] Dosage: 5, 10, 20 mg/kg,70 mg/kg Administration: orally once daily, 18 days Result: Prevented tumor growth at a dose of 5 mg/kg, and caused rapid and complete tumor regression in both groups of mice at a dose of 10 or 20 mg/kg. Significantly inhibited the proliferation and induced apoptosis of MV4-11 and K562 cells at a dose of 70 mg/kg.
References	[1]. Z-X Cao, et al. SKLB1028, a novel oral multikinase inhibitor of EGFR, FLT3 and Abl, displays exceptional activity in models of FLT3-driven AML and considerable potency in models of CML harboring Abl mutants. Leukemia. 2012 Aug;26(8):1892-5.

Density	1.3±0.1 g/cm3
Boiling Point	671.8±65.0 °C at 760 mmHg
Molecular Formula	C₂₄H₂₉N₉
Molecular Weight	443.55
Flash Point	360.1±34.3 °C
Exact Mass	443.254578
LogP	2.03
Vapour Pressure	0.0±2.1 mmHg at 25°C
Index of Refraction	1.707
Storage condition	2-8°C

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