| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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DS-437 (DS437) is a novel and potent dual PRMT5 and PRMT7 inhibitor with anticancer activity. It inhibits PRMT5/7 with IC50 of 6.0 uM, and is inactive against 29 other human protein-, DNA-, and RNA-methyltransferases.
| ln Vitro |
At equilibrium conditions (cofactor and substrate concentrations fixed at respective Km values), DS-437 can block the PRMT5-MEP50 complex's ability to methylate H4[1-24] peptide in a dose-dependent manner [1]. Its IC50 value is 5.9 ± 1.4 μM. The levels of CD8+ PD-1+ and total CD8+ T cells are raised by DS-437 [2].
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|---|---|
| ln Vivo |
There are some advantageous benefits of DS-437 (10 mg/kg; i.p.; 5 times weekly) on tumor growth inhibition. A more notable result was seen when DS-437 and anti-p185erbB2/neu antibody 4D5 were combined [1].
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| Animal Protocol |
Animal/Disease Models: Six to Ten weeks old female balb/c (Bagg ALBino) mouse (bearing CT26Her2 tumor cells)[1]
Doses: 10 mg/kg Route of Administration: ip; 5 times a week Experimental Results: Had some beneficial effects on inhibiting tumor growth. |
| References | |
| Additional Infomation |
See also: DS-437 (annotation moved to).
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| Molecular Formula |
C15H23N7O4S
|
|---|---|
| Molecular Weight |
397.45
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| Exact Mass |
397.153
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| CAS # |
1674364-87-4
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| PubChem CID |
122178085
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| Appearance |
Light brown to brown solid powder
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| Density |
1.7±0.1 g/cm3
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| Index of Refraction |
1.776
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| LogP |
0.16
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| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
505
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CCNC(=O)NCCSC[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O
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| InChi Key |
CACMCLIHCDTJHL-IDTAVKCVSA-N
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| InChi Code |
InChI=1S/C15H23N7O4S/c1-2-17-15(25)18-3-4-27-5-8-10(23)11(24)14(26-8)22-7-21-9-12(16)19-6-20-13(9)22/h6-8,10-11,14,23-24H,2-5H2,1H3,(H2,16,19,20)(H2,17,18,25)/t8-,10-,11-,14-/m1/s1
|
| Chemical Name |
1-[2-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-3-ethylurea
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| Synonyms |
DS437 DS 437 DS-437
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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) |
DMSO : ~125 mg/mL (~314.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5160 mL | 12.5802 mL | 25.1604 mL | |
| 5 mM | 0.5032 mL | 2.5160 mL | 5.0321 mL | |
| 10 mM | 0.2516 mL | 1.2580 mL | 2.5160 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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