Reagentia en instrumenten voor immunologie, celbiologie en moleculaire biologie.

H3B-6527 [1702259-66-2]

Afdrukken

Referentie HY-100491-5mg

Formaat : 5mg

Merk : MedChemExpress

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Description

H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC₅₀ of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC₅₀s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity^[1].

IC₅₀ & Target^[1]

FGFR4

<1.2 nM (IC₅₀)

FGFR1

320 nM (IC₅₀)

FGFR2

1290 nM (IC₅₀)

FGFR3

1060 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.9 nM Compound: 2; H3B-6527	Antiproliferative activity against mouse BaF3 cells harboring wild type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring wild type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
BaF3	IC₅₀	35.5 nM Compound: 2; H3B-6527	Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
BaF3	IC₅₀	60.3 nM Compound: 2; H3B-6527	Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]

In Vitro

H3B-6527 inhibits TAOK2, JNK2, and CSF1R with IC₅₀s of 690 nM, >10000 nM, and >10000 nM, respectively^[1].
H3B-6527 (10-10000 nM; 72 hours) results in a GI₅₀ value of 25 nM^[1].
H3B-6527 (10-10000 nM; 72 hours) leads cell death in HCC cell lines^[1].
H3B-6527 (0.1-1000 nM; 1 hour) decreases the levels of pERK1/2 in a dose-dependent manner with maximal inhibition occurring at 100 nM^[1].
H3B-6527 (1-1000 nM; 24 hours) causes a robust increase in CYP7A1 transcripts^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	Hepatocellular carcinoma (HCC) cell line Hep3B
Concentration:	10, 100, 1000, 10000 nM
Incubation Time:	72 hours
Result:	Resulted in a GI₅₀ value of 25 nM.

Apoptosis Analysis^[1]

Cell Line:	Hepatocellular carcinoma (HCC) cell line Hep3B
Concentration:	10, 100, 1000, 10000 nM
Incubation Time:	72 hours
Result:	Leaded cell death in HCC cell lines.

Western Blot Analysis^[1]

Cell Line:	Hepatocellular carcinoma (HCC) cell line Hep3B
Concentration:	0.1, 0.3, 1, 3, 10, 100, 1000 nM
Incubation Time:	1 hour
Result:	Decreased the levels of pERK1/2 in a dose-dependent manner with maximal inhibition occurring at 100 nM.

RT-PCR^[1]

Cell Line:	Hepatocellular carcinoma (HCC) cell line Hep3B
Concentration:	1, 10, 100, 1000 nM
Incubation Time:	24 hours
Result:	Caused a robust increase in CYP7A1 transcripts.

In Vivo

H3B-6527 (10-300 mg/kg; orally; twice-daily; for 15 days) significantly inhibits tumor growth at the 300 and 100 mg/kg and does not inhibit tumor growth at 30 and 10 mg/kg^[1].

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

Animal Model:	BALB/c nu/nu female mice approximately 8-week-old, weighing 18-20 g bearing Hep3B orthotopic xenografts in liver^[1]
Dosage:	10, 30, 100, 300 mg/kg
Administration:	Orally; twice-daily; for 15 days
Result:	Inhibited tumor growth at the 300 and 100 mg/kg twice-daily dose.

Essai clinique

Masse moléculaire

629.54

Formule

C₂₉H₃₄Cl₂N₈O₄

CAS No.

1702259-66-2

Appearance

Solid

Color

White to khaki

SMILES

C=CC(NC1=CC(N2CCN(CC)CC2)=CC=C1NC3=NC=NC(N(C(NC4=C(Cl)C(OC)=CC(OC)=C4Cl)=O)C)=C3)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 2.5 mg/mL (3.97 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	1.5885 mL	7.9423 mL	15.8846 mL
5 mM	---	---	---
10 mM	---	---	---

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.

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: ≥ 0.25 mg/mL (0.40 mM); Clear solution

This protocol yields a clear solution of ≥ 0.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.5 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: ≥ 0.25 mg/mL (0.40 mM); Clear solution

This protocol yields a clear solution of ≥ 0.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.5 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: ≥ 0.25 mg/mL (0.40 mM); Clear solution

This protocol yields a clear solution of ≥ 0.25 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 (2.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 98.0%

Fiche technique (277 KB) SDS (393 KB)

COA (249 KB) HNMR (299 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Joshi JJ, et al. H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven HepatocellularCarcinoma. Cancer Res. 2017 Dec 15;77(24):6999-7013. [Content Brief]

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Referentie HY-100491-5mg

Merk : MedChemExpress

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