BLU9931

Name: BLU9931
Brand: MedChemExpress
SKU: HY-12823
Rating: 5.0 (8 reviews)

Cat. No.: HY-12823 Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

BLU9931 is a potent, highly selective, and irreversible fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC₅₀ of 3 nM and a K_d of 6 nM. BLU9931 has significant antitumor activity.

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

BLU9931 Chemical Structure

CAS No. : 1538604-68-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 67	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 67	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 61	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 8 publication(s) in Google Scholar

7 Publications Citing Use of MCE BLU9931

•Int J Oncol. 2017 Nov;51(5):1611-1620. [Abstract]

: BLU9931 purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2017 Nov;51(5):1611-1620. [Abstract]; Western blot detection of the expression of related molecules including signal pathway (STAT3), apoptosis (cleaved caspase‑3), cell cycle (cyclin D1 and P27^kip1) and epithelial-mesenchymal transition (E-cadherin and vimentin) in HCT116 and SW620 cells when treated by the single and combination of 5-FU and Blu9931.

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View All Isoforms

FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

FGFR1

591 nM (IC₅₀)

FGFR2

493 nM (IC₅₀)

FGFR3

150 nM (IC₅₀)

FGFR4

3 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Hep 3B2	IC₅₀	0.058 μM Compound: 1a; BLU9931	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 33859803]
Hep 3B2	IC₅₀	0.288 μM Compound: BLU9931	Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by Cell Titer-Glo assay Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by Cell Titer-Glo assay	[PMID: 33218898]
Hep 3B2	IC₅₀	72 nM Compound: 15; BLU9931	Antiproliferative activity against human Hep3B cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human Hep3B cells incubated for 72 hrs by CCK8 assay	[PMID: 33030342]
HepG2	IC₅₀	5.458 μM Compound: BLU9931	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33618175]
Huh-7	IC₅₀	0.929 μM Compound: BLU9931	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay	[PMID: 34488024]
Huh-7	IC₅₀	327 nM Compound: 2; BLU9931	Inhibition of cell proliferation in human Huh-7 cells incubated for 72 hrs by Cell Titer-Glo luminescent assay Inhibition of cell proliferation in human Huh-7 cells incubated for 72 hrs by Cell Titer-Glo luminescent assay	[PMID: 35549181]
Huh-7	IC₅₀	5.386 μM Compound: BLU9931	Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33618175]
Huh-7	IC₅₀	84 nM Compound: 15; BLU9931	Antiproliferative activity against human Huh-7 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human Huh-7 cells incubated for 72 hrs by CCK8 assay	[PMID: 33030342]
MCF7	IC₅₀	2.34 μM Compound: 1; BLU9931	Antiproliferative activity against human MCF7 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay	[PMID: 28523108]
MDA-MB-231	IC₅₀	3.76 μM Compound: 1; BLU9931	Antiproliferative activity against human MDA-MB-231 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells expressing low levels of FGFR4 after 72 hrs by CCK8 assay	[PMID: 28523108]
MDA-MB-435	IC₅₀	0.039 μM Compound: 1a; BLU9931	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 33859803]
MDA-MB-453	IC₅₀	0.32 μM Compound: 1; BLU9931	Antiproliferative activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant after 72 hrs by CCK8 assay	[PMID: 28523108]
MDA-MB-453	IC₅₀	29 nM Compound: 2; BLU9931	Inhibition of cell proliferation in human MDA-MB-453 cells incubated for 72 hrs by Cell Titer-Glo luminescent assay Inhibition of cell proliferation in human MDA-MB-453 cells incubated for 72 hrs by Cell Titer-Glo luminescent assay	[PMID: 35549181]
NCI-H1299	IC₅₀	1.03 μM Compound: 1a; BLU9931	Antiproliferative activity against human H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 33859803]
SMMC-7721	IC₅₀	6.617 μM Compound: BLU9931	Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33618175]

In Vitro

BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, with EC₅₀s of 0.07 μM, 0.11 μM and 0.02 μM for Hep 3B, HuH7 and JHH7 cells, respectively^[1].
BLU9931 (0.3-300 nM; 1 hour; MDA-MB-453 and Hep 3B cells) treatment demonstrates potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 cells. BLU9931 shows dose-dependent inhibition of the signaling cascade downstream of FGFR4. BLU9931 exhibits potent inhibition of phosphorylation of the FGFR4 pathway components in Hep 3B cells. BLU9931 treatment leads to induction of caspase-3/7 activity, indicative of induction of apoptosis that results in inhibition of signaling downstream of FGFR4^[1].
BLU9931 (100 nM; 0 -24 hours; Hep 3B cells) treatment increases CYP7A1 mRNA expression and the expression of the proliferative marker EGR1 is inhibited^[1].

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

Western Blot Analysis^[1]

Cell Line:	MDA-MB-453 and Hep 3B cells
Concentration:	0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
Incubation Time:	1 hour
Result:	Demonstrated potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 and Hep 3B cells.

RT-PCR^[1]

Cell Line:	Hep 3B cells
Concentration:	100 nM
Incubation Time:	0 hour, 4 hours, 8 hour, 24 hours
Result:	Increased CYP7A1 mRNA expression. And the expression of the proliferative marker EGR1 was inhibited.

In Vivo

BLU9931 (10-100 mg/kg; oral administration; twice every day; for 21 days; mice) treatment demonstrates antitumor activity in HCC xenograft models^[1].

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

Animal Model:	Mice injected with Hep 3B cells^[1]
Dosage:	10 mg/kg, 30 mg/kg or 100 mg/kg
Administration:	Oral administration; twice every day; for 21 days
Result:	Resulted in dose-dependent growth inhibition of Hep 3B tumors. Prevented weight loss in a dose-dependent manner.

Molecular Weight

509.38

Formula

C₂₆H₂₂Cl₂N₄O₃

CAS No.

1538604-68-0

Appearance

Solid

Color

White to light yellow

SMILES

C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (163.59 mM; ultrasonic and warming and heat to 60°C; 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	1.9632 mL	9.8159 mL	19.6317 mL
5 mM	0.3926 mL	1.9632 mL	3.9263 mL
10 mM	0.1963 mL	0.9816 mL	1.9632 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 2.08 mg/mL (4.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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: 99.97%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (250 KB) HNMR (276 KB) RP-HPLC (255 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

References

[1]. Hagel M, et al. First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov. 2015 Apr;5(4):424-37. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9632 mL	9.8159 mL	19.6317 mL	49.0793 mL
	5 mM	0.3926 mL	1.9632 mL	3.9263 mL	9.8159 mL
	10 mM	0.1963 mL	0.9816 mL	1.9632 mL	4.9079 mL
	15 mM	0.1309 mL	0.6544 mL	1.3088 mL	3.2720 mL
	20 mM	0.0982 mL	0.4908 mL	0.9816 mL	2.4540 mL
	25 mM	0.0785 mL	0.3926 mL	0.7853 mL	1.9632 mL
	30 mM	0.0654 mL	0.3272 mL	0.6544 mL	1.6360 mL
	40 mM	0.0491 mL	0.2454 mL	0.4908 mL	1.2270 mL
	50 mM	0.0393 mL	0.1963 mL	0.3926 mL	0.9816 mL
	60 mM	0.0327 mL	0.1636 mL	0.3272 mL	0.8180 mL
	80 mM	0.0245 mL	0.1227 mL	0.2454 mL	0.6135 mL
	100 mM	0.0196 mL	0.0982 mL	0.1963 mL	0.4908 mL

BLU9931 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:

BLU99311538604-68-0BLU 9931BLU-9931FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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BLU9931

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BLU9931 Related Antibodies

7 Publications Citing Use of MCE BLU9931

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References

Customer Review

BLU9931 Related Antibodies

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Complete Stock Solution Preparation Table

BLU9931 Related Classifications

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