FPFT-2216

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

FPFT-2216 

FPFT-2216 是一种“分子胶水”化合物,可降解磷酸二酯酶 6D (PDE6D)、锌指转录因子 Ikaros (IKZF1)、Aiolos (IKZF3) 和酪蛋白激酶 1α (CK1α)。FPFT-2216 可用于癌症和炎症疾病的研究。

FPFT-2216

FPFT-2216 Chemical Structure

CAS No. : 2367619-87-0

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生物活性

FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease[1][2].

IC50 & Target[1]

PDE6D

 

CK1α

 

IKZF1

 

IKZF3

 

体外研究
(In Vitro)

FPFT-2216 (1 μM; 5 hours) is able to degrade PDE6D, in addition to its known targets IKZF1, IKZF3, and CK1α in MOLT4 cells[1].
FPFT-2216 (1 μM; 0 h, 2 h, 4 h, 6 h, 16 h, 24 h) shows complete degradation of PDE6D within 2 h, and the degradation of PDE6D persists for at least 24 h in MOLT4 cells[1].
FPFT-2216 (0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 1 μM; 4 h) exhibits over 50% degradation of PDE6D at a dose of 8 nM, while maximum degradation of PDE6D along with IKZF1, IKZF3, and CK1α at a dose of 200 nM in MOLT4 cells[1].
FPFT-2216 does not impede the growth of KRASG12C-dependent MIA PaCa-2 cells[1].
FPFT-2216 (10, 20, 40 µM; 14 or 24 h) highly up-regulates the production of IL-2 although it is less potent than that of Pomalidomide in Naive CD4+ T cells[2].
FPFT-2216 (10 µM; 14 or 24 h) degrades IKZF1 and CK-1α among ubiquitin–proteasomal degradative substrates of immunomodulatory drugs (IMiDs) in Naive CD4+ T cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MOLT4 cells
Concentration: 1 μM
Incubation Time: 0 h, 2 h, 4 h, 6 h, 16 h, 24 h
Result: Showed complete degradation of PDE6D within 2 h, and the degradation of PDE6D persisted for at least 24 h.

Western Blot Analysis[1]

Cell Line: MOLT4 cells
Concentration: 0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 1 μM
Incubation Time: 4 h
Result: Exhibited over 50% degradation of PDE6D at a dose of 8 nM, while maximum degradation of PDE6D along with IKZF1, IKZF3, and CK1α at a dose of 200 nM.

体内研究
(In Vivo)

FPFT-2216 (30 mg/kg; p.o. or i.p.) induces significant degradation of CK-1α, and IKZF1 in CRBNI391V mice[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CRBNI391V mice[2]
Dosage: 30 mg/kg (solubilized in 0.5% carboxymethylcellulose/sodium and 0.25% Tween 80)
Administration: p.o. or i.p.
Result: Induced significant degradation of CK-1α, and IKZF1.

分子量

292.31

Formula

C12H12N4O3S

CAS 号

2367619-87-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Teng M, et al. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. J Med Chem. 2022 Jan 13;65(1):747-756.

    [2]. Gemechu Y, et al. Humanized cereblon mice revealed two distinct therapeutic pathways of immunomodulatory drugs. Proc Natl Acad Sci U S A. 2018;115(46):11802-11807.

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