H3B-8800
Based on 1 Customer Validation
H3B-8800 is a potent and orally active SF3B splicing modulator. H3B-8800 direct interaction with the SF3b complex and shows anti-cancer activity. H3B-8800 has the potential for the research of acute myeloid leukemia (AML) with SF3B1 mutant.
For research use only. We do not sell to patients.
- Purity: 98.85%
- CAS No.: 1825302-42-8
- Formula: C31H45N3O6
- Molecular Weight:555.71
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Storage:Powder -20°C, 3 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
Biological Activity
SF3B splicing[1]
H3B-8800 (0.1-10000 nM; 72 h) inhibits cell growth in SF3B1-mutant cell line Panc05.04 cells[1].
H3B-8800 (0.1-10000 nM; 24 h) induces apoptosis in SF3B1-mutant cell line Panc05.04 cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SF3B1-mutant cell line Panc05.04 cells
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Concentration:0.1,1, 10, 100, 1000, 10000 nM
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Incubation Time:24 h
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Result:Induced apoptosis by increased caspase-3/7 cleavage in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 weeks, female NSG or CB17-SCID mice (K562 cells with SF3B1WT or SF3B1K700E)[1]
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Dosage:2, 4 mg/kg
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Administration:P.o.; daily
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Result:Resulted in antileukemic efficacy and splicing modulation in mice bearing AML patient-derived xenografts (PDXs) with a mutation in SF3B1 but had little effect in mice bearing SF3B1WT AML PDXs, significantly reduced leukemic burden relative in SF3B1K700E PDX.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1825302-42-8
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Appearance Solid
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Molecular Weight 555.71
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Formula C31H45N3O6
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SMILES
O=C(N1CCN(C)CC1)O[C@H]([C@](C)(O)CC[C@@H](O)C2)/C=C/[C@H](C)[C@H](OC2=O)/C(C)=C/C=C/[C@@H](C)C3=NC=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (179.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 1.7995 mL | 8.9975 mL | 17.9950 mL | 44.9875 mL |
| 5 mM | 0.3599 mL | 1.7995 mL | 3.5990 mL | 8.9975 mL | |
| 10 mM | 0.1799 mL | 0.8997 mL | 1.7995 mL | 4.4987 mL | |
| 15 mM | 0.1200 mL | 0.5998 mL | 1.1997 mL | 2.9992 mL | |
| 20 mM | 0.0900 mL | 0.4499 mL | 0.8997 mL | 2.2494 mL | |
| 25 mM | 0.0720 mL | 0.3599 mL | 0.7198 mL | 1.7995 mL | |
| 30 mM | 0.0600 mL | 0.2999 mL | 0.5998 mL | 1.4996 mL | |
| 40 mM | 0.0450 mL | 0.2249 mL | 0.4499 mL | 1.1247 mL | |
| 50 mM | 0.0360 mL | 0.1799 mL | 0.3599 mL | 0.8997 mL | |
| 60 mM | 0.0300 mL | 0.1500 mL | 0.2999 mL | 0.7498 mL | |
| 80 mM | 0.0225 mL | 0.1125 mL | 0.2249 mL | 0.5623 mL | |
| 100 mM | 0.0180 mL | 0.0900 mL | 0.1799 mL | 0.4499 mL |
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