NSC 370284

Names

[ Name ]:
NSC 370284

Biological Activity

[Description]:

NSC-370284 is a selective inhibitor of ten-eleven translocation 1 (TET1). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5. NSC-370284 has low cytotoxicity[1].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> STAT

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> STAT

[Target]

STAT3

STAT5

TET1

[In Vitro]

NSC-370284 (0-500 nM；24 h 或 48 h) 通过靶向 STAT3/5 抑制 MONOMAC-6、THP-1、KOCL-48 和 KASUMI-1 急性髓系白血病 (AML) 细胞活力。NSC-370284 显著下调 TET1 转录水平[1]。 Cell Viability Assay[1] Cell Line: AML cell lines including MONOMAC-6, THP-1, KOCL-48, and KASUMI-1 Concentration: 0, 25, 50, 200 or 500 nM Incubation Time: 24 h or 48 h Result: Showed inhibitory for AML cells viability and TET1 transcription.

[In Vivo]

NSC-370284 (2.5 mg/kg；腹腔注射，每天一次，持续 10 天) 改善了 MLL-AF9 急性髓系白血病 (AML) 小鼠模型外周血 (PB)、骨髓 (BM)、脾和肝组织的病理形态学[1]。 Animal Model: C57BL/6 (CD45.2) and B6.SJL (CD45.1) mice[1]. Dosage: 2.5 mg/kg. Administration: Intraperitoneal injection, once daily, for 10 days. Result: Significantly inhibited MLL-AF9 induced AML in secondary bone marrow transplantation (BMT) recipient mice.

[References]

[1]. Jiang X, et al. Targeted inhibition of STAT/TET1 axis as a therapeutic strategy for acute myeloid leukemia. Nat Commun. 2017 Dec 13;8(1):2099.

Chemical & Physical Properties

[ Density]:
1.276g/cm3

[ Boiling Point ]:
515.2ºC at 760mmHg

[ Molecular Formula ]:
C₂₁H₂₅NO₆

[ Molecular Weight ]:
387.42600

[ Flash Point ]:
265.4ºC

[ Exact Mass ]:
387.16800

[ PSA ]:
69.62000

[ LogP ]:
3.26980

[ Vapour Pressure ]:
3.09E-11mmHg at 25°C

[ Index of Refraction ]:
1.598

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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