| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
After just 12 hours of treatment, 50% of the protein (DC50) of FKBP12 PROTAC RC32 (RC32; 0.1-1000 nM; 12 hours) is degraded [1].
|
|---|---|
| ln Vivo |
In mouse organs treated for just one day, RC32 (RC32; i.p.; 30 mg/kg; twice daily; 1 day) suppresses the FKBP12 protein in all save the brain [1]. (Latoral: 60 mg/kg; twice daily; for a single day) lowers FKBP12 in mice by a considerable amount [1]. In the majority of the organs studied in 20 kg Bama pigs, RC32 (ip injection; 8 mg/kg; twice daily; for 2 days) efficiently breaks down the FKBP12 protein [1]. RC32 (ip injection; 8 mg/kg; twice daily; for 3 days) efficiently breaks down the heart, bone marrow, spleen,
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: Jurkat cells Tested Concentrations: 0.1, 1, 10, 100, 1000 nM Incubation Duration: 12 hrs (hours) Experimental Results: After only 12 hrs (hours) of treatment, protein degradation (DC50) was 50%, approximately 0.3 nM. |
| Animal Protocol |
Animal/Disease Models: Male and female mice [1]
Doses: 30 mg/kg Route of Administration: IP; FKBP12 in lungs and stomach[1]. Twice a day; 1 day Experimental Results: FKBP12 protein was degraded in most organs of treated mice after only 1 day of treatment. |
| References |
| Molecular Formula |
C75H107N7O20
|
|---|---|
| Molecular Weight |
1426.68700242043
|
| Exact Mass |
1425.757
|
| CAS # |
2375555-66-9
|
| PubChem CID |
146026069
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
5.8
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
23
|
| Rotatable Bond Count |
23
|
| Heavy Atom Count |
102
|
| Complexity |
2980
|
| Defined Atom Stereocenter Count |
15
|
| SMILES |
O(CCOCC1=CN(CCOCCOCCNC2=CC=CC3C(N(C(C=32)=O)C2C(NC(CC2)=O)=O)=O)N=N1)[C@@H]1CC[C@@H](C[C@@H](C)[C@@H]2CC([C@@H](C=C(C)[C@H]([C@H](C([C@H](C)C[C@H](C)C=CC=CC=C(C)[C@H](C[C@@H]3CC[C@@H](C)[C@@](C(C(N4CCCC[C@H]4C(=O)O2)=O)=O)(O)O3)OC)=O)OC)O)C)=O)C[C@H]1OC |c:64,66,t:53,68|
|
| InChi Key |
XCSUEITWRRFFMN-SJQMKIJVSA-N
|
| InChi Code |
InChI=1S/C75H107N7O20/c1-45-17-12-11-13-18-46(2)61(94-8)41-54-24-22-51(7)75(93,102-54)69(87)73(91)81-29-15-14-21-58(81)74(92)101-62(42-59(83)47(3)38-50(6)67(86)68(96-10)66(85)49(5)37-45)48(4)39-52-23-26-60(63(40-52)95-9)100-36-35-99-44-53-43-80(79-78-53)30-32-98-34-33-97-31-28-76-56-20-16-19-55-65(56)72(90)82(71(55)89)57-25-27-64(84)77-70(57)88/h11-13,16-20,38,43,45,47-49,51-52,54,57-58,60-63,67-68,76,86,93H,14-15,21-37,39-42,44H2,1-10H3,(H,77,84,88)/b13-11+,17-12+,46-18+,50-38+/t45-,47-,48-,49-,51-,52+,54+,57?,58+,60-,61+,62+,63-,67-,68+,75-/m1/s1
|
| Chemical Name |
(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-12-[(2R)-1-[(1S,3R,4R)-4-[2-[[1-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethyl]triazol-4-yl]methoxy]ethoxy]-3-methoxycyclohexyl]propan-2-yl]-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
|
| Synonyms |
FKBP12 PROTAC RC32; FKBP12 PROTAC RC32
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| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~7.01 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (0.70 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 + to the above solution and mix evenly; then add 450 μL of 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7009 mL | 3.5046 mL | 7.0092 mL | |
| 5 mM | 0.1402 mL | 0.7009 mL | 1.4018 mL | |
| 10 mM | 0.0701 mL | 0.3505 mL | 0.7009 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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