JNJ-16241199
Based on 1 Customer Validation
JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.
For research use only. We do not sell to patients.
- Purity: 99.05%
- CAS No.: 604769-01-9
- Formula: C19H19N5O4S
- Molecular Weight:413.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Apoptosis Compound Library
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Biological Activity
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HDAC1 3.3 nM (IC50) |
HDAC8 23 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
39 nM
Compound: 1, R306465
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Antiproliferative activity against human A2780 cells
Antiproliferative activity against human A2780 cells
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[PMID: 19906529] |
| HeLa | IC50 |
6 nM
Compound: 1, R306465
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Inhibition of HDAC in human HeLa cells extractt
Inhibition of HDAC in human HeLa cells extractt
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[PMID: 19906529] |
JNJ-16241199 (R306465) (10-40 mpk/day for 28 days, p.o.) inhibits the growth of A2780 ovarian, H460 lung and HCT116 colon carcinomas orthotopic xenograft tumor models [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human A2780 ovarian carcinoma cells
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Concentration:0, 0.1, 0.3, 1 μM
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Incubation Time:24 h or 48 h
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Result:Decreased in S phase at 300 nM, with a parallel increase in G1 phase, but increased in the sub-G1 fraction of cells at the 1 μM after 24 h.
Increased in sub-G1 phase at all active concentrations starting from 100 nM after 48 h.
JNJ-16241199 inhibits the primary human mammary epithelial cell (HMEC) proliferation with the IC50 of 32 nM, and is insensitive to quiescent, non-proliferative HMEC cells (IC50 = 7815 nM) [1].
JNJ-16241199 (0.1, 0.3, 1 μM, 24-48 h) induces apoptosis and inhibits angiogenesis in A2780 cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human A2780, H460 and HCT116 orthotopic xenograft tumor models[1]
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Dosage:10-40 mpk/day for 28 days
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Administration:Oral gavage (p.o.)
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Result:Induced H3 acetylation and p21waf1, cip1 promoter activity in A2780 ovarian tumour tissue.
Decreased tumour volume in three orthotopic xenograft tumor models.
Reached maximal decrease in final tumour volume to 76–87% in human A2780 orthotopic xenograft tumor models.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 604769-01-9
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Appearance Solid
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Molecular Weight 413.45
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Formula C19H19N5O4S
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Color White to off-white
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SMILES
O=S(N(CC1)CCN1C2=NC=C(C(NO)=O)C=N2)(C3=CC=C4C(C=CC=C4)=C3)=O
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Synonyms
R306465
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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 : 11.67 mg/mL (28.23 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. 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 (273 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)
- Korean - KR (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 | 2.4187 mL | 12.0934 mL | 24.1867 mL | 60.4668 mL |
| 5 mM | 0.4837 mL | 2.4187 mL | 4.8373 mL | 12.0934 mL | |
| 10 mM | 0.2419 mL | 1.2093 mL | 2.4187 mL | 6.0467 mL | |
| 15 mM | 0.1612 mL | 0.8062 mL | 1.6124 mL | 4.0311 mL | |
| 20 mM | 0.1209 mL | 0.6047 mL | 1.2093 mL | 3.0233 mL | |
| 25 mM | 0.0967 mL | 0.4837 mL | 0.9675 mL | 2.4187 mL |
JNJ-16241199 Related Classifications
HY-10226 Related Classifications
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