FR901464

Name: FR901464
Brand: MedChemExpress
SKU: HY-16212
Rating: 4.5 (1 reviews)

Cat. No.: HY-16212 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

FR901464 is a potent spliceosome inhibitor with prominent anti-tumor and anti-cancer effects.

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

FR901464 Chemical Structure

CAS No. : 146478-72-0

Size	Price	Stock	Quantity
1 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1920	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 3850	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 6150	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 9800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
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Description

FR901464 is a potent spliceosome inhibitor with prominent anti-tumor and anti-cancer effects^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.0013 μM Compound: FR-901464	Cytotoxicity against human A549 cells after 72 hrs by XTT colorimetric assay Cytotoxicity against human A549 cells after 72 hrs by XTT colorimetric assay	[PMID: 18788726]
A549	GI₅₀	1 nM Compound: FR901464	Antiproliferative activity against human A549 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay	10.1039/C0MD00179A
DU-145	GI₅₀	1.05 nM Compound: 4, FR901464	Antiproliferative activity against human DU145 cells assessed as growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human DU145 cells assessed as growth inhibition measured after 48 hrs by MTT assay	[PMID: 23517093]
HCT-116	GI₅₀	1 nM Compound: FR901464	Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay	10.1039/C0MD00179A
HEK293	IC₅₀	0.58 μM Compound: 4, FR901464	Inhibition of Pre-mRNA splicing in human HEK293 cells using p32-labeled CDC14-15 pre-mRNA by exonjunction complex (EJC) immunoprecipitation assay Inhibition of Pre-mRNA splicing in human HEK293 cells using p32-labeled CDC14-15 pre-mRNA by exonjunction complex (EJC) immunoprecipitation assay	[PMID: 23517093]
MCF7	IC₅₀	0.0018 μM Compound: FR-901464	Cytotoxicity against human MCF7 cells after 72 hrs by XTT colorimetric assay Cytotoxicity against human MCF7 cells after 72 hrs by XTT colorimetric assay	[PMID: 18788726]
MCF7	GI₅₀	1 nM Compound: FR901464	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay	10.1039/C0MD00179A
MCF7	GI₅₀	1.1 nM Compound: 1; FR901464	Cytotoxicity against human MCF7 cells incubated for 7 to 10 days by MTS assay Cytotoxicity against human MCF7 cells incubated for 7 to 10 days by MTS assay	[PMID: 33974423]
MDA-MB-231	GI₅₀	2.1 nM Compound: 4, FR901464	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 48 hrs by MTT assay	[PMID: 23517093]
P388	GI₅₀	1 nM Compound: FR901464	Antiproliferative activity against mouse P388 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay Antiproliferative activity against mouse P388 cells assessed as growth inhibition after 24 to 72 hrs by MTS assay	10.1039/C0MD00179A
SK-OV-3	GI₅₀	1.06 nM Compound: 4, FR901464	Antiproliferative activity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human SKOV3 cells assessed as growth inhibition measured after 48 hrs by MTT assay	[PMID: 23517093]

In Vitro

FR901464 (10-20 ng/ml; 6-24 hours) inhibits the growth of murine solid tumors, Colon 38 carcinoma and Meth A fibrosarcoma. FR901464 induces characteristic G1 and G2/M phase arrest in the cell cycle and internucleosomal degradation of genomic DNA with the same kinetics as activation of SV40 promoter-dependent cellular transcription in M-8 tumor cells^[1].
FR901464 (1-10 ng/ml; 16 hours) suppresses the transcription of some inducible endogenous genes but not house keeping genes in M-8 cells^[1].
FR901464 exhibits potent anticancer activity^[1].

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

Molecular Weight

507.62

Formula

C₂₇H₄₁NO₈

CAS No.

146478-72-0

Appearance

Solid

Color

White to off-white

SMILES

O[C@H]([C@H](O1)/C=C/C(C)=C/C[C@H](O[C@@H]2C)[C@H](C[C@H]2NC(/C=C\[C@H](C)OC(C)=O)=O)C)[C@@]3(C[C@]1(O)C)CO3

Structure Classification

Alkaloids

Initial Source

Microorganisms

Pseudomonas sp

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (197.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9700 mL	9.8499 mL	19.6998 mL
5 mM	0.3940 mL	1.9700 mL	3.9400 mL
10 mM	0.1970 mL	0.9850 mL	1.9700 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (271 KB) SDS (557 KB)

COA (247 KB) HNMR (279 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. II. Activities against experimental tumors in mice and mechanism of action. J Antibiot (Tokyo). 1996 Dec;49(12):1204-11. [Content Brief]

[2]. Arun K Ghosh, et al. Enantioselective total syntheses of FR901464 and spliceostatin A and evaluation of splicing activity of key derivatives. J Org Chem. 2014 Jun 20;79(12):5697-709. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9700 mL	9.8499 mL	19.6998 mL	49.2494 mL
	5 mM	0.3940 mL	1.9700 mL	3.9400 mL	9.8499 mL
	10 mM	0.1970 mL	0.9850 mL	1.9700 mL	4.9249 mL
	15 mM	0.1313 mL	0.6567 mL	1.3133 mL	3.2833 mL
	20 mM	0.0985 mL	0.4925 mL	0.9850 mL	2.4625 mL
	25 mM	0.0788 mL	0.3940 mL	0.7880 mL	1.9700 mL
	30 mM	0.0657 mL	0.3283 mL	0.6567 mL	1.6416 mL
	40 mM	0.0492 mL	0.2462 mL	0.4925 mL	1.2312 mL
	50 mM	0.0394 mL	0.1970 mL	0.3940 mL	0.9850 mL
	60 mM	0.0328 mL	0.1642 mL	0.3283 mL	0.8208 mL
	80 mM	0.0246 mL	0.1231 mL	0.2462 mL	0.6156 mL
	100 mM	0.0197 mL	0.0985 mL	0.1970 mL	0.4925 mL

FR901464 Related Classifications

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:

FR901464146478-72-0FR 901464FR-901464Otherscancerchemotherapyspliceosomeanti-tumorM-8Inhibitorinhibitorinhibit

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FR901464

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