Itacnosertib hydrochloride
Based on 1 Customer Validation
Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, ACVR1 (ALK2, IC50=8 nM) and JAK2 (IC50=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.43%
- CAS. Nr.: 2409543-84-4
- Formel: C26H29ClN8O
- Molecular Weight:505.01
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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ACVR1 8 nM (IC50) |
JAK2 8540 nM (IC50) |
Itacnosertib hydrochloride (0-200 nM, 24-48 h) arrests the cell cycle of MOLM-13, MOLM-14 and MV4-11 at G1/G0 phase, inhibits the proliferation of acute myeloid leukemia (AML) cells, IC50s for MOLM-13, MOLM-14 and MV4-11 (FLT3-mutated AML cells) are 6.4, 1.2 and 1.3 nM, respectively. Itacnosertib hydrochloride inhibits the AML FLT3-wildtype cell with IC50 > 100 nM[2].
Itacnosertib hydrochloride inhibits the activation of FLT3 and ACVR1 downstream signaling pathways, inhibits serine biosynthesis and amino acid transport pathways[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-13, MOLM-14 and MV4-11
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Concentration:0-1000 nM
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Incubation Time:24-48 h
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Result:Inhibited the phosphorylation of STAT5, MKK3, ERK, PI3K, AKT, mTOR, p-4E-BP1, p-S6K and SMAD1/5.
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Cell Line:MOLM-13, MOLM-14 and MV4-11
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Concentration:0-200 nM
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Incubation Time:24-48 h
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Result:Arrested the cell cycle at subG1 phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse MOLM-13 xenograft models[2]
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Dosage:50-200 mg/kg
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Administration:po, once weekly for 5-6 weeks
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Result:Inhibited the leukemia growth, prolonged the mice survival.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2409543-84-4
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Appearance Solid
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Molecular Weight 505.01
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Formel C26H29ClN8O
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Color Off-white to light brown
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SMILES
CN1CCN(C2=CC=C(NC3=NC=CC(NC4=CC=CN=C4C5=NC=CC=C5)=N3)C=C2OC)CC1.[H]Cl
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Synonyms
TP-0184 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 5.56 mg/mL (11.01 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)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 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)
Verweise
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 (sealed storage, away from moisture). 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 | 1.9802 mL | 9.9008 mL | 19.8016 mL | 49.5040 mL |
| 5 mM | 0.3960 mL | 1.9802 mL | 3.9603 mL | 9.9008 mL | |
| 10 mM | 0.1980 mL | 0.9901 mL | 1.9802 mL | 4.9504 mL |
Itacnosertib hydrochloride Related Classifications
HY-109179A Related Classifications
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