SF2523 | PI3K Inhibitor | AmBeed-信号通路专用抑制剂

SF2523 {[allProObj[0].p_purity_real_show]}

货号：A390649

SF2523能够阻断 BRD4 与 MYCN 启动子 PS1/PS2 的结合。

SF2523 化学结构
CAS号：1174428-47-7

SF2523 3D分子结构
CAS号：1174428-47-7

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PI3K 亚型比较

产品名称	C2β ↓ ↑	p110α ↓ ↑	p110β ↓ ↑	p110γ ↓ ↑	p110δ ↓ ↑	PI3K ↓ ↑	Vps34 ↓ ↑	其他靶点	纯度
A66	+ C2β, IC50: 462 nM	++ p110α, IC50: 32 nM							99%+
Taselisib	+ C2β, IC50: 292 nM	++++ PI3Kα, Ki: 0.29 nM	+++ PI3Kβ, Ki: 9.1 nM	++++ PI3Kγ, Ki: 0.97 nM	++++ PI3Kδ, Ki: 0.12 nM		+ hVps34, IC50: 374 nM		99%+
Gedatolisib		++++ PI3Kα, IC50: 0.4 nM		+++ PI3Kγ, IC50: 5.4 nM				mTOR	99%
HS-173		++++ PI3Kα , IC50: 0.8 nM							99%+
Serabelisib		+++ PI3Kα, IC50: 21 nM							99%+
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	99%
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	98%
AS-252424		+ PI3Kα, IC50: 935 nM		++ PI3Kγ, IC50: 33 nM					99%
Alpelisib		+++ PI3Kα, IC50: 5 nM							99%+
AS-604850		+ PI3Kα, IC50: 4.5 μM		+ PI3Kγ, IC50: 0.25 μM					99%
SF2523		++ PI3Kα, IC50: 34 nM		++ PI3Kγ, IC50: 158 nM				DNA-PK,mTOR	99%+
Inavolisib		++++ PI3K alpha, IC50: 0.038 nM							99%+
Bimiralisib		++++ PI3Kα, Kd: 1.5 nM	+++ PI3Kβ, Kd: 11 nM	++ PI3Kγ, Kd: 25 nM	++ PI3Kδ, Kd: 25 nM			mTOR	99%+
GSK1059615		++++ PI3Kα, IC50: 0.4 nM	++++ PI3Kβ, IC50: 0.6 nM	+++ PI3Kγ, IC50: 5 nM	++++ PI3Kδ, IC50: 2 nM			mTOR	98%
GSK2636771			✔						99%
Fimepinostat		+++ PI3Kα, IC50: 19 nM	++ PI3Kβ, IC50: 54 nM		++ PI3Kδ, IC50: 39 nM				99%+
VS-5584		++++ PI3Kα, IC50: 2.6 nM	+++ PI3Kβ, IC50: 21 nM	++++ PI3Kγ, IC50: 3.0 nM	++++ PI3Kδ, IC50: 2.7 nM			mTOR	98%
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				98+%
PI-103		++++ p110α, IC50: 2 nM	++++ p110β, IC50: 3 nM	+++ p110γ, IC50: 15 nM	++++ p110δ, IC50: 3 nM			DNA-PK,mTOR	99%+
PI-3065			+ p110β, IC50: 1078 nM		+++ p110δ, IC50: 15 nM				99%+
Voxtalisib		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	99%+
AZD-8835		+++ PI3Kα, IC50: 6.2 nM	+ PI3Kβ, IC50: 431 nM	++ PI3Kγ, IC50: 90 nM	+++ PI3Kδ, IC50: 5.7 nM				99%
Pilaralisib analogue		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 36 nM	+++ PI3Kγ, IC50: 23 nM	++ PI3Kδ, IC50: 36 nM				99%+
ZSTK474		+++ PI3Kα, IC50: 16 nM	++ PI3Kβ, IC50: 44 nM	++ PI3Kγ, IC50: 49 nM	+++ PI3Kδ, IC50: 4.6 nM	++ PI3K, IC50: 37 nM			98%
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				98%
TGX-221			+++ p110β, IC50: 5 nM		++ p110δ, IC50: 0.1 μM				99%+
PF-04691502		++++ PI3Kα, Ki: 1.8 nM	++++ PI3Kβ, Ki: 2.1 nM	++++ PI3Kγ, Ki: 1.9 nM	++++ PI3Kδ, Ki: 1.6 nM			mTOR	98+%
GDC-0084		++++ PI3Kα, Ki app: 2 nM	++ PI3Kβ, Ki app: 46 nM	+++ PI3Kγ, Ki app: 10 nM	++++ PI3Kδ, Ki app: 3 nM			mTOR	99%+
Buparlisib		++ p110α, IC50: 52 nM	+ p110β, IC50: 166 nM	+ p110γ, IC50: 262 nM	++ p110δ, IC50: 116 nM		+ Vps34, IC50: 2.4 μM	mTOR	98%
LY294002		+ p110α, IC50: 0.5 μM	+ p110β, IC50: 0.97 μM		+ p110δ, IC50: 0.57 μM			DNA-PK	99%+
AZD 6482		+ PI3Kα, IC50: 870 nM	+++ PI3Kβ, IC50: 10 nM		++ PI3Kδ, IC50: 80 nM			DNA-PK	99%+
Pictilisib		++++ p110α, IC50: 3 nM	++ p110β, IC50: 33 nM	++ p110γ, IC50: 75 nM	++++ p110δ, IC50: 3 nM			mTOR	99%+
PKI-402		++++ PI3Kα, IC50: 2 nM	+++ PI3Kβ, IC50: 7 nM	+++ PI3Kγ, IC50: 16 nM	+++ PI3Kδ, IC50: 14 nM			mTOR	98%
Copanlisib		++++ PI3Kα, IC50: 0.5 nM	++++ PI3Kβ, IC50: 3.7 nM	+++ PI3Kγ, IC50: 6.4 nM	++++ PI3Kδ, IC50: 0.7 nM				99%+
Omipalisib		++++ p110α, Ki: 0.019 nM	++++ p110β, Ki: 0.13 nM	++++ p110γ, Ki: 0.06 nM	++++ p110δ, Ki: 0.024 nM				99%+
Izorlisib		+++ PI3Kα, IC50: 14 nM	++ PI3Kβ, IC50: 0.12 μM	++ PI3Kγ, IC50: 36 nM	+ PI3Kδ, IC50: 0.50 μM				99%+
AZD8186		++ PI3Kα, IC50: 35 nM	++++ PI3Kβ, IC50: 4 nM		+++ PI3Kδ, IC50: 12 nM				99%
KU-0060648		++++ PI3Kα, IC50: 4 nM	++++ PI3Kβ, IC50: 0.5 nM	+ PI3Kγ, IC50: 0.59 μM	++++ PI3Kδ, IC50: 0.1 nM			DNA-PK	98%
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	98%+
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					98+%
BGT226 maleate		++++ PI3Kα, IC50: 4 nM	++ PI3Kβ, IC50: 63 nM	++ PI3Kγ, IC50: 38 nM				mTOR	99%+
TG 100713		++ PI3Kα, IC50: 165 nM	+ PI3Kβ, IC50: 215 nM	++ PI3Kγ, IC50: 50 nM	+++ PI3Kδ, IC50: 24 nM				98%+
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	98+%
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				98%
PIK-90		+++ PI3Kα, IC50: 11 nM	+ PI3Kβ, IC50: 350 nM	+++ PI3Kγ, IC50: 18 nM	++ PI3Kδ, IC50: 58 nM				99%+
PIK-294			+ p110β, IC50: 490 nM	++ p110γ, IC50: 160 nM	+++ p110δ, IC50: 10 nM				99%+
Duvelisib			++++ PI3Kβ, Ki: 1564 pM	++ PI3Kγ, Ki: 243 pM	++++ PI3Kδ, Ki: 23 pM				99%+
GDC-0326		++++ PI3Kα, Ki: 0.2 nM	++ PI3Kβ, Ki: 26.6 nM	+++ PI3Kγ, Ki: 10.2 nM	++++ PI3Kδ, Ki: 4 nM				98%
Quercetin Dihydrate			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM				95%
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Sirtuin,PKC,Src	95%
Leniolisib		+ PI3Kα, IC50: 0.244 μM	+ PI3Kβ, IC50: 0.424 μM	+ PI3Kγ, IC50: 2.23 μM	+++ PI3Kδ, IC50: 0.011 μM			DNA-PK	99%+
PIK-108			✔						99%
Eganelisib				+++ PI3Kγ, IC50: 16 nM					99%+
CAY10505				✔					99%
IPI-3063					++++ p110δ, IC50: 2.5 nM				99%
Nemiralisib					++++ PI3Kδ, pKi: 9.9				99%+
PF-4989216		++++ p110α, IC50: 2 nM		++ p110γ, IC50: 65 nM	++++ p110δ, IC50: 1 nM				99%+
PIK-75 HCl		+++ p110α, IC50: 5.8 nM		++ p110γ, IC50: 76 nM	+ p110δ, IC50: 0.51 μM			DNA-PK	99%+
Tenalisib				++ PI3Kγ, IC50: 33.2 nM	++ PI3Kδ, IC50: 24.5 nM				98%
Acalisib					+++ p110δ, IC50: 14 nM				99%+
Umbralisib					+++ PI3Kδ, IC50: 22.2 nM				99%+
AMG319				+ PI3Kγ, IC50: 850 nM	+++ PI3Kδ, IC50: 18 nM				99%
IC-87114				+ PI3Kγ, IC50: 29 μM	+ PI3Kδ, IC50: 0.5 μM				99%+
Idelalisib				++ p110γ, IC50: 89 nM	++++ p110δ, IC50: 2.5 nM				98%
PIK-293				+ p110γ, IC50: 10 μM	+ p110δ, IC50: 0.24 μM				99%+
Vps34-PIK-III					+ PI3Kδ, IC50: 1.2μM		+++ Vps34, IC50: 0.018μM		99%+
GSK2292767					✔				98%
Seletalisib				+ PI3Kγ, IC50: 282 nM	+++ PI3Kδ, IC50: 12 nM				99%+
P110δ-IN-1					++++ P110δ, IC50: 0.6 nM				99%
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				99%
SRX3207		+ PI3K alpha, IC50: 244 nM		+ PI3K gamma, IC50: 9790 nM	+ PI3K delta, IC50: 388 nM			Syk	98%
Parsaclisib HCl					++++ PI3Kδ, IC50: 1 nM				98%
IHMT-PI3Kδ-372					+++ PI3Kδ, IC50: 14 nM				98%
Trigonelline						✔		Akt	99%+
Wortmannin						++++ PI3K, IC50: 3 nM		DNA-PK,MLCK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		Akt,PTEN	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		CDK,Akt,ATM/ATR	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	99%+
Cinobufagine						✔		Akt	99%
α-Linolenic acid						✔			97% (GC)
MTX-211						✔		EGFR	98%
PI3K/mTOR Inhibitor-2						++++ PI3K, IC50: 3.4 nM		mTOR	99%+
SPP-86						✔			99%+
(E)-Akt inhibitor-IV						✔			98%
Vps34-IN-1							++ Vps34, IC50: 25 nM		98%
SAR405							++++ Vps34, IC50: 1.2 nM		98+%
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	98%
Vps34-IN-4							+++ VPS34, IC50: 15 nM		98%+
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

SF2523 生物活性

靶点

p110γ

PI3Kγ, IC50:158 nM
p110α

PI3Kα, IC50:34 nM
mTOR

mTOR, IC50:280 nM
DNA-PK

DNA-PK, IC50:9 nM
BET

BRD4, IC50:241 nM

描述

The phosphatidylinositol 3-kinase (PI3K) pathway is a major focus for drug development in various cancer due to its function as a key regulator of cell growth and survival. The bromodomain and extraterminal domain (BET) family of epigenetic “reader” proteins, including BRDT, BRD2, BRD3, and BRD4, play important roles in histone acetylation-dependent transcriptional regulation. SF2523 is a highly selective and potent inhibitor of PI3K with IC₅₀s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively^[1]. In vitro, SF2523 decreased LPS- or IL4-induced MΘ polarization. At 500 nM, SF2523 significantly decreased mRNA expression of IL6 and iNos in LPS induced Bone marrow–derived macrophages (BMDMs) and gene expression of Arg, Tgfb, Vegf, Mmr, Ym1, and Fizz1 in IL4-induced BMDMs^[2]. In vivo, s.c. xenograft model of MYCN-amplified neuroblastoma in immunocompromised mice treated with SF2523 (50 mg/kg, three times a week) showed a significant reduction of tumor volume compared with vehicle-treated group, without gross toxicity^[1].

作用机制

The structure of the BRD4 BD1–SF2523 complex reveals a characteristic four-helix bundle fold of BD1, with SF2523 occupying a deep hydrophobic pocket at one of the open ends of the bundle.

SF2523 细胞实验

Cell Line Bone marrow-derived macrophages (BMDMs) Neuroblastoma SKNBE2 cells Human macrophages Neuroblastoma SKNBE2 cells HD-MB03 cells DAOY cells HD-MB03 cells DAOY cells	Concentration	Treated Time	Description	References
Bone marrow-derived macrophages (BMDMs)	500 nM or 1 µM	1 hour	SF2523 significantly decreased the mRNA expression of IL6 and iNos in LPS induced BMDMs and gene expression of Arg, Tgfb, Vegf, Mmr, Ym1, and Fizz1 in IL4-induced BMDMs.	Mol Cancer Ther. 2019 Jun;18(6):1036-1044.
Neuroblastoma SKNBE2 cells	5 µM	24 hours	To evaluate the effect of SF2523 on MYCN expression, results showed that SF2523 significantly reduced MYCN mRNA levels by approximately sevenfold.	Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):E1072-E1080.
Human macrophages	500 nM	24 hours	SF2523 increased LC3B-II levels and decreased SQSTM1 protein levels, indicating it can overcome HIV-imposed autophagy inhibition and induce autophagy.	J Biol Chem. 2018 Apr 20;293(16):5808-5820.
Neuroblastoma SKNBE2 cells	5 µM	30 minutes	To evaluate the effect of SF2523 on the PI3K signaling pathway, results showed that SF2523 decreased MYCN and Cyclin D1 protein levels and inhibited phosphorylation of AKT at Ser473.	Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):E1072-E1080.
HD-MB03 cells	5.8 µM	48 hours	SF2523 inhibited HD-MB03 cell proliferation with IC50 of 5.8 μM, and in combination with MDB5 significantly decreased MYCN, p-AKT, and cyclin D1 expression while increasing Bax expression	Biomaterials. 2021 Nov;278:121138.
DAOY cells	12.6 µM	48 hours	SF2523 inhibited DAOY cell proliferation with IC50 of 12.6 μM, and in combination with MDB5 significantly decreased MYCN, p-AKT, and cyclin D1 expression while increasing Bax expression	Biomaterials. 2021 Nov;278:121138.
HD-MB03 cells	5.14 µM (IC50)	48 hours	Evaluate the inhibitory effect of SF2523 on HD-MB03 cell proliferation, showing an IC50 of 5.14 μM.	J Control Release. 2023 Feb;354:80-90.
DAOY cells	12.6 µM (IC50)	48 hours	Evaluate the inhibitory effect of SF2523 on DAOY cell proliferation, showing an IC50 of 12.6 μM.	J Control Release. 2023 Feb;354:80-90.

Cell Line

Bone marrow-derived macrophages (BMDMs) Neuroblastoma SKNBE2 cells Human macrophages Neuroblastoma SKNBE2 cells HD-MB03 cells DAOY cells HD-MB03 cells DAOY cells

Concentration

Treated Time

Description

References

Bone marrow-derived macrophages (BMDMs)

500 nM or 1 µM

1 hour

SF2523 significantly decreased the mRNA expression of IL6 and iNos in LPS induced BMDMs and gene expression of Arg, Tgfb, Vegf, Mmr, Ym1, and Fizz1 in IL4-induced BMDMs.

Mol Cancer Ther. 2019 Jun;18(6):1036-1044.

Neuroblastoma SKNBE2 cells

5 µM

24 hours

To evaluate the effect of SF2523 on MYCN expression, results showed that SF2523 significantly reduced MYCN mRNA levels by approximately sevenfold.

Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):E1072-E1080.

Human macrophages

500 nM

24 hours

SF2523 increased LC3B-II levels and decreased SQSTM1 protein levels, indicating it can overcome HIV-imposed autophagy inhibition and induce autophagy.

J Biol Chem. 2018 Apr 20;293(16):5808-5820.

Neuroblastoma SKNBE2 cells

5 µM

30 minutes

To evaluate the effect of SF2523 on the PI3K signaling pathway, results showed that SF2523 decreased MYCN and Cyclin D1 protein levels and inhibited phosphorylation of AKT at Ser473.

Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):E1072-E1080.

HD-MB03 cells

5.8 µM

48 hours

SF2523 inhibited HD-MB03 cell proliferation with IC50 of 5.8 μM, and in combination with MDB5 significantly decreased MYCN, p-AKT, and cyclin D1 expression while increasing Bax expression

Biomaterials. 2021 Nov;278:121138.

DAOY cells

12.6 µM

48 hours

SF2523 inhibited DAOY cell proliferation with IC50 of 12.6 μM, and in combination with MDB5 significantly decreased MYCN, p-AKT, and cyclin D1 expression while increasing Bax expression

Biomaterials. 2021 Nov;278:121138.

HD-MB03 cells

5.14 µM (IC50)

48 hours

Evaluate the inhibitory effect of SF2523 on HD-MB03 cell proliferation, showing an IC50 of 5.14 μM.

J Control Release. 2023 Feb;354:80-90.

DAOY cells

12.6 µM (IC50)

48 hours

Evaluate the inhibitory effect of SF2523 on DAOY cell proliferation, showing an IC50 of 12.6 μM.

J Control Release. 2023 Feb;354:80-90.

SF2523 动物实验

Species NSG mice NSG mice Mice (C57Bl/6, Balb/c, FVB PyMT+) Nude mice	Animal Model Orthotopic SHH-MB tumor model Xenograft and orthotopic MB tumor models Lewis lung carcinoma (LLC), CT26 colon adenocarcinoma, B16 melanoma, Panc02 pancreatic cancer, PyMT+ spontaneous breast cancer Subcutaneous xenograft model of MYCN-amplified neuroblastoma	Administration	Dosage	Frequency	Description	References
NSG mice	Orthotopic SHH-MB tumor model	Intravenous injection	20 mg/kg	Every 3 days for 3 weeks	COG-133-NPs loaded with SF2523 significantly increased drug concentration in the cerebellum at 6 h (0.272 ± 0.007 ng/mg) and 24 h (0.08 ± 0.001 ng/mg), significantly inhibiting tumor growth	Biomaterials. 2021 Nov;278:121138.
NSG mice	Xenograft and orthotopic MB tumor models	Intravenous injection	20 mg/kg	Every third day for two weeks	Evaluate the antitumor efficacy of SF2523 in MB tumor models, showing significant reduction in tumor growth and prolonged animal survival.	J Control Release. 2023 Feb;354:80-90.
Mice (C57Bl/6, Balb/c, FVB PyMT+)	Lewis lung carcinoma (LLC), CT26 colon adenocarcinoma, B16 melanoma, Panc02 pancreatic cancer, PyMT+ spontaneous breast cancer	Subcutaneous injection	40 mg/kg	Thrice weekly for 4 weeks	SF2523 significantly suppressed tumor growth and metastasis, reduced MDSC infiltration, and increased CD8+ T cell infiltration and activity.	Mol Cancer Ther. 2019 Jun;18(6):1036-1044.
Nude mice	Subcutaneous xenograft model of MYCN-amplified neuroblastoma	Intraperitoneal injection	50 mg/kg	Three times a week until tumors were harvested	To evaluate the effect of SF2523 on tumor growth, results showed that SF2523 significantly reduced tumor volume with no gross toxicity to the mice.	Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):E1072-E1080.

Species

NSG mice NSG mice Mice (C57Bl/6, Balb/c, FVB PyMT+) Nude mice

Animal Model

Orthotopic SHH-MB tumor model Xenograft and orthotopic MB tumor models Lewis lung carcinoma (LLC), CT26 colon adenocarcinoma, B16 melanoma, Panc02 pancreatic cancer, PyMT+ spontaneous breast cancer Subcutaneous xenograft model of MYCN-amplified neuroblastoma

Administration

Dosage

Frequency

Description

References

NSG mice

Orthotopic SHH-MB tumor model

Intravenous injection

20 mg/kg

Every 3 days for 3 weeks

COG-133-NPs loaded with SF2523 significantly increased drug concentration in the cerebellum at 6 h (0.272 ± 0.007 ng/mg) and 24 h (0.08 ± 0.001 ng/mg), significantly inhibiting tumor growth

Biomaterials. 2021 Nov;278:121138.

NSG mice

Xenograft and orthotopic MB tumor models

Intravenous injection

20 mg/kg

Every third day for two weeks

Evaluate the antitumor efficacy of SF2523 in MB tumor models, showing significant reduction in tumor growth and prolonged animal survival.

J Control Release. 2023 Feb;354:80-90.

Mice (C57Bl/6, Balb/c, FVB PyMT+)

Lewis lung carcinoma (LLC), CT26 colon adenocarcinoma, B16 melanoma, Panc02 pancreatic cancer, PyMT+ spontaneous breast cancer

Subcutaneous injection

40 mg/kg

Thrice weekly for 4 weeks

SF2523 significantly suppressed tumor growth and metastasis, reduced MDSC infiltration, and increased CD8+ T cell infiltration and activity.

Mol Cancer Ther. 2019 Jun;18(6):1036-1044.

Nude mice

Subcutaneous xenograft model of MYCN-amplified neuroblastoma

Intraperitoneal injection

50 mg/kg

Three times a week until tumors were harvested

To evaluate the effect of SF2523 on tumor growth, results showed that SF2523 significantly reduced tumor volume with no gross toxicity to the mice.

Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):E1072-E1080.

SF2523 参考文献

SF2523 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL

SF2523 技术信息

CAS号	1174428-47-7
分子式	C₁₉H₁₇NO₅S
分子量	371.41
SMILES Code	O=C1C2=C(C(C3=CC=C(OCCO4)C4=C3)=CS2)OC(N5CCOCC5)=C1
MDL No.	MFCD31382129

别名
运输	蓝冰
InChI Key	BYTKNUOMWLJVNQ-UHFFFAOYSA-N
Pubchem ID	44180156

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 30 mg/mL(80.77 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

靶点

靶点	数值

p110γ	PI3Kγ, IC50:158 nM
p110α	PI3Kα, IC50:34 nM
mTOR	mTOR, IC50:280 nM
DNA-PK	DNA-PK, IC50:9 nM
BET	BRD4, IC50:241 nM

SF2523 {[allProObj[0].p_purity_real_show]}

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靶点	p110γ PI3Kγ, IC50:158 nM p110α PI3Kα, IC50:34 nM mTOR mTOR, IC50:280 nM DNA-PK DNA-PK, IC50:9 nM BET BRD4, IC50:241 nM
描述	The phosphatidylinositol 3-kinase (PI3K) pathway is a major focus for drug development in various cancer due to its function as a key regulator of cell growth and survival. The bromodomain and extraterminal domain (BET) family of epigenetic “reader” proteins, including BRDT, BRD2, BRD3, and BRD4, play important roles in histone acetylation-dependent transcriptional regulation. SF2523 is a highly selective and potent inhibitor of PI3K with IC₅₀s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively^[1]. In vitro, SF2523 decreased LPS- or IL4-induced MΘ polarization. At 500 nM, SF2523 significantly decreased mRNA expression of IL6 and iNos in LPS induced Bone marrow–derived macrophages (BMDMs) and gene expression of Arg, Tgfb, Vegf, Mmr, Ym1, and Fizz1 in IL4-induced BMDMs^[2]. In vivo, s.c. xenograft model of MYCN-amplified neuroblastoma in immunocompromised mice treated with SF2523 (50 mg/kg, three times a week) showed a significant reduction of tumor volume compared with vehicle-treated group, without gross toxicity^[1].
作用机制	The structure of the BRD4 BD1–SF2523 complex reveals a characteristic four-helix bundle fold of BD1, with SF2523 occupying a deep hydrophobic pocket at one of the open ends of the bundle.

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