H3B-6527
Based on 1 Customer Validation
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.
- Purity: 98.0%
- CAS No.: 1702259-66-2
- Formula: C29H34Cl2N8O4
- Molecular Weight:629.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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FGFR4 <1.2 nM (IC50) |
FGFR1 320 nM (IC50) |
FGFR2 1290 nM (IC50) |
FGFR3 1060 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| BaF3 | IC50 |
0.9 nM
Compound: 2; H3B-6527
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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
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[PMID: 38348819] |
| BaF3 | IC50 |
35.5 nM
Compound: 2; H3B-6527
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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
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[PMID: 38348819] |
| BaF3 | IC50 |
60.3 nM
Compound: 2; H3B-6527
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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
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[PMID: 38348819] |
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.
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Cell Line:Hepatocellular carcinoma (HCC) cell line Hep3B
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Concentration:10, 100, 1000, 10000 nM
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Incubation Time:72 hours
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Result:Resulted in a GI50 value of 25 nM.
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Cell Line:Hepatocellular carcinoma (HCC) cell line Hep3B
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Concentration:10, 100, 1000, 10000 nM
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Incubation Time:72 hours
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Result:Leaded cell death in HCC cell lines.
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Cell Line:Hepatocellular carcinoma (HCC) cell line Hep3B
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Concentration:0.1, 0.3, 1, 3, 10, 100, 1000 nM
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Incubation Time:1 hour
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Result:Decreased the levels of pERK1/2 in a dose-dependent manner with maximal inhibition occurring at 100 nM.
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Cell Line:Hepatocellular carcinoma (HCC) cell line Hep3B
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Concentration:1, 10, 100, 1000 nM
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Incubation Time:24 hours
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Result:Caused a robust increase in CYP7A1 transcripts.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nu/nu female mice approximately 8-week-old, weighing 18-20 g bearing Hep3B orthotopic xenografts in liver[1]
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Dosage:10, 30, 100, 300 mg/kg
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Administration:Orally; twice-daily; for 15 days
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Result:Inhibited tumor growth at the 300 and 100 mg/kg twice-daily dose.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1702259-66-2
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Appearance Solid
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Molecular Weight 629.54
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Formula C29H34Cl2N8O4
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Color White to khaki
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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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