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| 25mg |
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Purity: ≥98%
LLY-284 (LLY284) is a negative control and tool compound for LLY-283. It is a diastereomer of LLY-283 but was much less active. LLY-283 (LLY283) is the first-in-class and selective SAM-competitive inhibitor of PRMT5 (protein arginine methyltransferase 5) with antitumor activity. LLY-283 inhibited PRMT5 enzymatic activity in vitro and in cells with IC50 values of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 also showed antitumor activity in mouse xenografts when dosed orally and can serve as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. PRMT5 is ubiquitously expressed in most tissues and its expression has been shown to be elevated in several cancers including breast cancer, gastric cancer, glioblastoma, and lymphoma. PRMTs binds to the lysine or arginine residues of substrate proteins via the substrate binding groove and SAM via the cofactor binding site.
| Molecular Formula |
C17H18N4O4
|
|---|---|
| Molecular Weight |
342.36
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| Exact Mass |
342.132
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| CAS # |
2226515-75-7
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| Related CAS # |
LLY-283;2040291-27-6
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| PubChem CID |
136213035
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| Appearance |
White to off-white solid powder
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| LogP |
0.2
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
464
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1=CC=C(C=C1)[C@@H]([C@@H]2[C@H]([C@H]([C@@H](O2)N3C=CC4=C(N=CN=C43)N)O)O)O
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| InChi Key |
WWOOWAHTEXIWBO-CNUKPYSBSA-N
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| InChi Code |
InChI=1S/C17H18N4O4/c18-15-10-6-7-21(16(10)20-8-19-15)17-13(24)12(23)14(25-17)11(22)9-4-2-1-3-5-9/h1-8,11-14,17,22-24H,(H2,18,19,20)/t11-,12-,13+,14+,17+/m0/s1
|
| Chemical Name |
(2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(S)-hydroxy(phenyl)methyl]oxolane-3,4-diol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9209 mL | 14.6045 mL | 29.2090 mL | |
| 5 mM | 0.5842 mL | 2.9209 mL | 5.8418 mL | |
| 10 mM | 0.2921 mL | 1.4605 mL | 2.9209 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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