FL118 (Synonyms: 10,11-(Methylenedioxy)-20(S)-camptothecin)

目录号: HY-12486 纯度: 99.40%: FAQs
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摩尔计算器

FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin)，一种喜树碱 (Camptothecin; HY-16560) 类似物，是一种口服有效的 survivin 抑制剂。FL118 与 DDX5 (p68) 结合，去磷酸化并降解 DDX5。FL118 可用于癌症的研究。

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FL118 Chemical Structure

CAS No. : 135415-73-5

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生物活性
纯度 & 产品资料
参考文献

生物活性

FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin (HY-16560) analogue, is a potent and orally active survivin inhibitor. FL118 binds to oncoprotein DDX5 (p68) to dephosphorylates and degrades DDX5. FL118 can be used for the research of cancer^[1]^[2].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
2008	IC₅₀	37.28 nM Compound: 4; FL118	Antiproliferative activity against human 2008 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human 2008 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
A549	IC₅₀	0.083 μM Compound: 24; FL118, Table 2, cpd 7	Cytotoxicity against human A549 cells incubated for 48 hrs by by SpectraMax M5 microplate reader analysis Cytotoxicity against human A549 cells incubated for 48 hrs by by SpectraMax M5 microplate reader analysis	[PMID: 34175539]
Bel-7402	IC₅₀	21.75 nM Compound: 4; FL118	Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
H69AR	IC₅₀	6.29 nM Compound: 4; FL118	Antiproliferative activity against human NCI-H69AR cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human NCI-H69AR cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
HepG2	IC₅₀	10.64 nM Compound: 4; FL118	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
HL-60	IC₅₀	0.027 μM Compound: 5z	Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells	[PMID: 8410981]
MCF7	IC₅₀	63.26 nM Compound: 4; FL118	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
NCI-H446	IC₅₀	18.54 nM Compound: 4; FL118	Antiproliferative activity against Irinotecan-resistant human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against Irinotecan-resistant human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
NCI-H446	IC₅₀	6.61 nM Compound: 4; FL118	Antiproliferative activity against etoposide/cisplatin combination-resistant human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against etoposide/cisplatin combination-resistant human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
NCI-H446	IC₅₀	8.87 nM Compound: 4; FL118	Antiproliferative activity against human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human NCI-H446 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
NCI-H69	IC₅₀	15.81 nM Compound: 4; FL118	Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human NCI-H69 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
SH-SY5Y	IC₅₀	24.19 nM Compound: 4; FL118	Antiproliferative activity against human SH-SY5Y cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SH-SY5Y cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
SW-620	IC₅₀	0.93 nM Compound: 4; FL118	Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]
U-87MG ATCC	IC₅₀	108.57 nM Compound: 4; FL118	Antiproliferative activity against human U87 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human U87 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35932565]

体外研究
(In Vitro)

FL118 (0-200 nM; 24, 48 and 72 h ) inhibits the cell proliferation of ES-2 and SK-O-V₃ cells^[1].
FL118 (0-100 nM; 0 and 24 h) inhibits the migration of ES-2 and SK-O-V₃ cells^[1].
FL118 (0-100 nM; 48 h) affects the expression level of cytoglobin (CYGB)^[1].
FL118 (10 and 100 nM; 48 h) inhibits PI3K/AKT/mTOR signaling pathway, and affects the expression level of vimentin and E-cadherin in ovarian cancer cells^[1].
FL118 (0-100 nM; 6 and 24 h) dephosphorylates and degrades DDX5^[2].
FL118 (0-500 nM; 24, 48, 72 h) regulates survivin, McL-1, XIAP, cIAP2, c-MYc and mKras by regulating DDX5^[2].
FL118 (0-1 μM, 24 h) shows significant cytotoxic activity against the three tumor cell lines (A549, MDA-MB-231, and RM-1 cells)^[3].
FL118 (0-10 nM, 48 h) increases the production of PARP cleavage, and induces apoptosis in A549^[3].
FL118 (0-10 nM, 48 h) arrests A549 cells mainly at the G2/M phase^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	ES-2 and SK-O-V₃ cell lines
Concentration:	10 and 100 nM
Incubation Time:	48 h
Result:	Effectively inhibited the activation of PI3K/AKT/mTOR signaling pathway in ovarian cancer cells and also inhibited the migration of ES-2 and SK-O-V₃ cells.

Cell Migration Assay ^[1]

Cell Line:	ES-2 and SK-O-V₃ cell lines
Concentration:	0, 10 and 100 nM
Incubation Time:	0 and 24 h
Result:	Inhibited the migration of ES-2 and SK-O-V₃ cells dose-dependenly.

RT-PCR^[1]

Cell Line:	ES-2 and SK-O-V₃ cell lines
Concentration:	0, 10 and 100 nM
Incubation Time:	48 h
Result:	Promoted CYGB expression.

Cell Proliferation Assay^[1]

Cell Line:	ES-2 and SK-O-V₃ cell lines
Concentration:	0, 1, 10, 50, 100 and 200 nM
Incubation Time:	24, 48 and 72 h
Result:	Inhibited the cell proliferation of ES-2 and SK-O-V₃ cells time- and dose-dependently.

Western Blot Analysis^[2]

Cell Line:	SW620 and Mia Paca-2
Concentration:	0, 10 and 100 nM
Incubation Time:	6 and 24 h
Result:	Induced dephosphorylation of DDX5 through the ubiquitin-proteasome degradation pathway and degraded DDX5 time-dependently.

Western Blot Analysis^[2]

Cell Line:	PDAC Panc1, CRC HCT-8, SW620, Mia Paca-2, Panc-1, HCT-8 cell lines
Concentration:	0, 10, 100 and 500 nM
Incubation Time:	24, 48, 72 h
Result:	Controled the expression of survivin, Mcl-1, XIAP, cIAP2, c-Myc and mKras by regulated DDX5, as an upstream master regulator in cancer development and malignant networks.

Cell Cytotoxicity Assay^[3]

Cell Line:	A549, MDA-MB-231, RM-1
Concentration:	0-1 μM
Incubation Time:	24 h
Result:	Showed cytotoxicity in A-549 (human lung carcinoma), MDA-MB-231 (human breast carcinoma) and RM-1 (mouse prostate carcinoma), with IC₅₀ values of 8.94 ± 1.54 , 24.73 ± 13.82, and 69.19 ± 8.34 nM, respectively.

Apoptosis Analysis^[3]

Cell Line:	A549 cells
Concentration:	0, 2.5, 5, 10 nM
Incubation Time:	48 h
Result:	Resulted in the downregulation of survivin. Increased the production of PARP cleavage in a concentration-dependent manner, which is the hallmark of apoptosis. Induced apoptosis in A549.

Cell Cycle Analysis^[3]

Cell Line:	A549 cells
Concentration:	0, 2.5, 5, 10 nM
Incubation Time:	48 h
Result:	Increased G2/M cell population in a concentration-dependent manner, and arrested A549 cells mainly at the G2/M phase.

体内研究
(In Vivo)

FL118 (5 and 10 mg/kg; p.o. once a week for 20 days) inhibits antitumor activity^[1].
FL118 (0-1.5 mg/kg, i.p. once every other day for five times) effectively eliminates human colon and head-and-neck tumors that acquire irinotecan or topotecan resistance^[4].
FL118 (1.5 mg/kg, i.v. once) exhibits favorable pharmacokinetics profiles^[4].
Pharmacokinetic Parameters of FL118 in female SCID mice^[4].

Sample	FaDu	SW620	Plasma
T_1/2 (hr)	6.852	12.75	1.788
T_max (hr)	0.167	0.167	0.167
C_max (ng/g, mL)	115	158	43
AUC (hr*ng/g)	413	842	82
AUC_∞ (hr*ng/g)	448	897	104
AUC% Extrap (%)	7.74	6.17	21.7
Vz (g/kg) (ml/kg)	33052	30742	36849
Cl (g/hr/kg) (ml/hr/kg)	3343	1671	14287

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Fmale BALB/c nude mice^[1]
Dosage:	5 and 10 mg/kg
Administration:	Oral gavage; 5 mg/kg for once a week; 10 mg/kg for once a week; for 20 days
Result:	Showed better antitumor activity than topotecan and dose-dependenly suppressed the growth of ES-2 tumors by upregulating the expression level of CYGB.

Animal Model:	SCID (severe combined immunodeficiency) mice bearing human SW620 (colon) and FaDu (head-and-neck) xenograft tumors (ten-week-old, female, 20-25 g, 5 mice per cage)^[4]
Dosage:	0, 0.75, 1, 1.5 mg/kg
Administration:	IP, once every other day for five times as one cycle (If tumors relapse, mice were treated with FL118 for second or third cycles)
Result:	Eliminated human xenograft tumors that acquired irinotecan or topotecan resistance, and was also effective after multiple cycles of treatment without the generation of FL118 resistance.

Animal Model:	SCID (severe combined immunodeficiency) mice bearing human SW620 (colon) and FaDu SCID mice bearing human SW620 (colon) and FaDu (head-and-neck) xenograft tumors (ten-week-old, female, 20-25 g, 5 mice per cage)^[4]
Dosage:	1.5 mg/kg
Administration:	IV, once
Result:	Exhibited favorable pharmacokinetics profiles.

分子量

392.36

Formula

C₂₁H₁₆N₂O₆

CAS 号

135415-73-5

性状

固体

颜色

Light brown to brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 1 mg/mL (2.55 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5487 mL	12.7434 mL	25.4868 mL
5 mM	---	---	---
10 mM	---	---	---

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* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

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纯度 & 产品资料

纯度: 99.40%

选择批次：

Data Sheet (618 KB) SDS (420 KB)

COA (200 KB) HNMR (469 KB) RP-HPLC (205 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Zhao H, et al. FL118, a novel anticancer compound, inhibits proliferation and migration of ovarian cancer cells via up-regulation of cytoglobin in vivo and in vitro[J]. Translational Cancer Research, 2017, 6(6):1294-1304.

[2]. Ling X, et al. FL118, acting as a 'molecular glue degrader', binds to dephosphorylates and degrades the oncoprotein DDX5 (p68) to control c-Myc, survivin and mutant Kras against colorectal and pancreatic cancer with high efficacy. Clin Transl Med. 2022 May;12(5):e881. [Content Brief]

[3]. Wu G, et al. Synthesis of novel 10,11-methylenedioxy-camptothecin glycoside derivatives and investigation of their anti-tumor effects in vivo. RSC Adv. 2019 Apr 9;9(20):11142-11150. [Content Brief]

[4]. Ling X, et, al. FL118, a novel camptothecin analogue, overcomes irinotecan and topotecan resistance in human tumor xenograft models. Am J Transl Res. 2015 Oct 15;7(10):1765-81. [Content Brief]

FL118 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO

1 mM

2.5487 mL

12.7434 mL

25.4868 mL

63.7170 mL

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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沪(浦)应急管危经许[2021]201709(QFYS)

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FL118 (Synonyms: 10,11-(Methylenedioxy)-20(S)-camptothecin)

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