FR-β ligand 1

目录号: HY-172935: Data Sheet 产品使用指南
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FR-β ligand 1 (III) 是一种靶向叶酸受体的配体，具有抗肿瘤活性、高选择性，和强亲和力。

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FR-β ligand 1 Chemical Structure

CAS No. : 863869-78-7

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生物活性
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参考文献

生物活性

FR-β ligand 1 (III), a folate receptor-targeting ligand, possesses antitumor activity, high selectivity, and stronger affinity for folate receptor^[1].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	GI₅₀	8.98 x 10^-7 M Compound: 6	Cytotoxicity of compound against 786-0 renal cancer cell line Cytotoxicity of compound against 786-0 renal cancer cell line	[PMID: 16078850]
A2780	IC₅₀	14.2 nM Compound: 2	Antiproliferative activity against human A2780 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human A2780 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
CCRF-CEM	EC₅₀	1100 nM Compound: 6	Growth inhibitory activity against CCRF-CEM human lymphoblastic leukemia cells Growth inhibitory activity against CCRF-CEM human lymphoblastic leukemia cells	[PMID: 16078850]
CCRF-CEM	EC₅₀	18000 nM Compound: 6	Growth inhibitory activity against MTX resistant CCRF-CEM human lymphoblastic leukemia cells with decreased polyglutamylation Growth inhibitory activity against MTX resistant CCRF-CEM human lymphoblastic leukemia cells with decreased polyglutamylation	[PMID: 16078850]
CCRF-CEM	EC₅₀	3050 nM Compound: 6	Growth inhibitory activity against MTX resistant subline of CCRF-CEM human lymphoblastic leukemia cells Growth inhibitory activity against MTX resistant subline of CCRF-CEM human lymphoblastic leukemia cells	[PMID: 16078850]
CCRF-CEM	EC₅₀	8100 nM Compound: 6	Growth inhibitory activity against resistant CCRF-CEM human lymphoblastic leukemia cells with decreased uptake of MTX Growth inhibitory activity against resistant CCRF-CEM human lymphoblastic leukemia cells with decreased uptake of MTX	[PMID: 16078850]
HL-60	GI₅₀	6.56 x 10^-6 M Compound: 6	Cytotoxicity of compound aganist HL-60 leukemia cell line Cytotoxicity of compound aganist HL-60 leukemia cell line	[PMID: 16078850]
IGROV-1	IC₅₀	1.12 nM Compound: 1	Antiproliferative activity against human IGROV1 cells expressing human FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human IGROV1 cells expressing human FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay	[PMID: 29425443]
IGROV-1	IC₅₀	3.6 nM Compound: 3	Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells	[PMID: 18680275]
IGROV-1	IC₅₀	3.6 nM Compound: 4	Growth inhibition of human IGROV1 cells expressing RFC, FRalpha and PCFT after 96 hrs Growth inhibition of human IGROV1 cells expressing RFC, FRalpha and PCFT after 96 hrs	[PMID: 20085328]
IGROV-1	IC₅₀	4.37 nM Compound: 2	Antiproliferative activity against wild type human IGROV1 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against wild type human IGROV1 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	5.21 nM Compound: 2	Antiproliferative activity against human IGROV1 cells harboring non targeted control shRNA sequence after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human IGROV1 cells harboring non targeted control shRNA sequence after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	> 1000 nM Compound: 1	Antiproliferative activity against human IGROV1 cells expressing human FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay Antiproliferative activity against human IGROV1 cells expressing human FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay	[PMID: 29425443]
IGROV-1	IC₅₀	> 1000 nM Compound: 2	Antiproliferative activity against FRalpha knockout human IGROV1 KD10 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against FRalpha knockout human IGROV1 KD10 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	> 1000 nM Compound: 2	Antiproliferative activity against FRalpha knockout human IGROV1 KD4 cells after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against FRalpha knockout human IGROV1 KD4 cells after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
IGROV-1	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells in presence of folic acid Antiproliferative activity against human RFC and FRalpha expressing human IGROV1 cells in presence of folic acid	[PMID: 18680275]
K562	GI₅₀	3.98 x 10^-7 M Compound: 6	Cytotoxicity of compound against K-564 leukemia cell line Cytotoxicity of compound against K-564 leukemia cell line	[PMID: 16078850]
KB	IC₅₀	1 nM Compound: 1	Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay	[PMID: 29425443]
KB	IC₅₀	1.9 nM Compound: 2	Inhibition of GARFTase in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Inhibition of GARFTase in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 32503687]
KB	IC₅₀	1.9 nM Compound: 3	Antiproliferative activity against human RFC and FRalpha expressing human KB cells Antiproliferative activity against human RFC and FRalpha expressing human KB cells	[PMID: 18680275]
KB	IC₅₀	1.9 nM Compound: 4	Growth inhibition of human KB cells expressing RFC, FRalpha and PCFT after 96 hrs Growth inhibition of human KB cells expressing RFC, FRalpha and PCFT after 96 hrs	[PMID: 20085328]
KB	IC₅₀	5.71 nM Compound: 2	Inhibition of GARFTase in human KB cells assessed as incorporation of [14C]-glycine into [14C]-formyl GAR incubated 30 mins prior to [14C]-glycine addition measured after 16 hrs by radiometric assay in presence of azaserin Inhibition of GARFTase in human KB cells assessed as incorporation of [14C]-glycine into [14C]-formyl GAR incubated 30 mins prior to [14C]-glycine addition measured after 16 hrs by radiometric assay in presence of azaserin	[PMID: 24256410]
KB	IC₅₀	6.8 nM Compound: 3	Inhibition of GARFTase in human KB cells assessed as inhibition of [14C]glycine incorporation into [14C]formylGAR in presence of azaserine Inhibition of GARFTase in human KB cells assessed as inhibition of [14C]glycine incorporation into [14C]formylGAR in presence of azaserine	[PMID: 18680275]
KB	IC₅₀	6.8 μM Compound: 4	Inhibition of GARFtase in human KB cells assessed as [14C]glycine incorporation in to [14C]FGAR in folate free RPMI medium with 2 nM LCV by in-situassay Inhibition of GARFtase in human KB cells assessed as [14C]glycine incorporation in to [14C]FGAR in folate free RPMI medium with 2 nM LCV by in-situassay	[PMID: 20085328]
KB	IC₅₀	> 1000 nM Compound: 1	Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay	[PMID: 29425443]
KB	IC₅₀	> 1000 nM Compound: 2	Inhibition of GARFTase in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs in presence of folic acid by Cell-Titer Blue assay Inhibition of GARFTase in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs in presence of folic acid by Cell-Titer Blue assay	[PMID: 32503687]
KB	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against human RFC and FRalpha expressing human KB cells in presence of folic acid Antiproliferative activity against human RFC and FRalpha expressing human KB cells in presence of folic acid	[PMID: 18680275]
R2	IC₅₀	213 nM Compound: 2	Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay	[PMID: 24256410]
R2	IC₅₀	213 nM Compound: 2	Inhibition of GARFTase in Chinese Hamster MTXRII-OuaR2-4 R2 cells expressing human PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Inhibition of GARFTase in Chinese Hamster MTXRII-OuaR2-4 R2 cells expressing human PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 32503687]
R2	IC₅₀	213 nM Compound: 2b	Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay	[PMID: 24111942]
R2	IC₅₀	> 1000 nM Compound: 1	Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay	[PMID: 29425443]
R2	IC₅₀	> 1000 nM Compound: 2	Antiproliferative activity in Chinese hamster R2 cells deficient in RFC, PCFT, and FRalpha assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Antiproliferative activity in Chinese hamster R2 cells deficient in RFC, PCFT, and FRalpha assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 29701475]
R2	IC₅₀	> 1000 nM Compound: 2	Inhibition of GARFTase in Chinese Hamster MTXRII-OuaR2-4/RFC/FRalpha/PCFT-null R2 cells assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay Inhibition of GARFTase in Chinese Hamster MTXRII-OuaR2-4/RFC/FRalpha/PCFT-null R2 cells assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay	[PMID: 32503687]
R2	IC₅₀	> 1000 nM Compound: 3	Antiproliferative activity against human RFC expressing Chinese hamster R2 cells Antiproliferative activity against human RFC expressing Chinese hamster R2 cells	[PMID: 18680275]
SR	GI₅₀	6.09 x 10^-7 M Compound: 6	Cytotoxicity of compound against SR leukemia cell line Cytotoxicity of compound against SR leukemia cell line	[PMID: 16078850]
SW-620	GI₅₀	3.81 x 10^-6 M Compound: 6	Cytotoxicity of compound against SW-620 colon cancer cell line Cytotoxicity of compound against SW-620 colon cancer cell line	[PMID: 16078850]

分子量

455.46

Formula

C₂₂H₂₅N₅O₆

CAS 号

863869-78-7

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.

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

[1]. Lixiao Guo, et al. Design and Synthesis of FR-β Targeting Chimeric Molecules for Reprogramming Tumor-Associated Macrophages Using 6-Substituted Pyrrolo[2,3- d]pyrimidines as Targeting Ligands. J Med Chem. 2025 Apr 24;68(8):8295-8309. [Content Brief]

FR-β ligand 1 相关分类

摩尔计算器
稀释计算器

The molarity calculator equation

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

质量		浓度		体积		分子量 *
	=		×		×

The dilution calculator equation

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)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
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.

Keywords:

FR-β ligand 1863869-78-7AntifolateInhibitorinhibitorinhibit

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

FR-β ligand 1

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