1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. H3B-6527

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.

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

H3B-6527 Chemical Structure

H3B-6527 Chemical Structure

CAS No. : 1702259-66-2

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Based on 1 publication(s) in Google Scholar

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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)

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.
Molecular Weight

629.54

Formula

C29H34Cl2N8O4

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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 --- --- ---
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.

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Purity & Documentation

Purity: ≥98.0%

References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5885 mL 7.9423 mL 15.8846 mL 39.7115 mL
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H3B-6527 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.

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Product Name:
H3B-6527
Cat. No.:
HY-100491
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