Cat. No.: HY-172935

FR-β ligand 1

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

For research use only. We do not sell to patients.

CAS No.: 863869-78-7
Formula: C₂₂H₂₅N₅O₆
Molecular Weight:455.46

Storage:

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

Data Sheet (266 KB)

FR-β ligand 1 Chemical Structure

CAS No.: 863869-78-7

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Biological Activity
- Description
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

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

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	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]
CCRF-CEM	EC₅₀	18 μM 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]
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	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	>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]
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	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	>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 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	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: 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]
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	1.9 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	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	>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]
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	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	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	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	>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	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	>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]
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]
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	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	>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	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	>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]
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]

Chemical Information

CAS No. 863869-78-7
Molecular Weight 455.46
Formula C₂₂H₂₅N₅O₆
SMILES

NC(NC1=O)=NC2=C1C=C(CCCCC3=CC=C(C=C3)C(N[C@H](C(O)=O)CCC(O)=O)=O)N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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