JNJ-64619178 (Synonyms: Onametostat) |
| Catalog No.GC19465 |
JNJ-64619178 (Onametostat) est un inhibiteur sélectif, actif par voie orale et pseudo-irréversible de la protéine arginine méthyltransférase 5 (PRMT5) avec une IC50 de 0,14 nM. JNJ-64619178 a une activité puissante dans le cancer du poumon.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2086772-26-9
Sample solution is provided at 25 µL, 10mM.
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JNJ-64619178 is a PRMT5 inhibitor with high selectivity and potency (PRMT5-MEP-50, IC50=0.14 nM), good pharmacokinetic properties and safety.
JNJ-64619178 can be combined with a SAM binding pocket to inhibit the function of PRMT/MEP50 in a time-dependent manner. Various cell lines exhibited different degrees of sensitivity to JNJ-64619178, indicating that JNJ-64619178 inhibits PRMT5 mainly by genomic rather than general targeted cytotoxicity [1].
The methylation of SMD1/3 protein can be selectively and effectively prevented by oral administration of 10 mg/kg JNJ-64619178 per day. SMD1/3 is a key component of the splice and a substrate for PRMT5/MEP50. In the biomarker-driven human small cell lung cancer xenograft model (NCI-H1048), JNJ-64619178 can cause tumor regression and prolong tumor growth inhibition after termination of administration [1].
Reference:
[1] Dirk Brehmer, et al. 108th Annu Meet Am Assoc Cancer Research
| Cas No. | 2086772-26-9 | SDF | |
| Synonymes | Onametostat | ||
| Chemical Name | (1S,2R,3S,5R)-3-(2-(2-amino-3-bromoquinolin-7-yl)ethyl)-5-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol | ||
| Canonical SMILES | BrC1=C(N)N=C(C=C(CC[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C(N=CN=C4N)=C4C=C3)C2)C=C5)C5=C1 | ||
| Formula | C22H23BrN6O2 | M.Wt | 483.36 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0689 mL | 10.3443 mL | 20.6885 mL |
| 5 mM | 0.4138 mL | 2.0689 mL | 4.1377 mL |
| 10 mM | 0.2069 mL | 1.0344 mL | 2.0689 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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