| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
dCBP-1 is a novel, potent and selective heterobifunctional and PROTAC degrader of p300/CBP with potential anticancer activity. It is highly potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression.
| ln Vitro |
In MM1S cells, dCBP-1 (10–1000 nM; 6 hours) nearly entirely degrades p300/CBP. In additional multiple myeloma cell lines tested, such as MM1R, KMS-12-BM, and KMS34 cells, dCBP-1 can also transduce nearly complete p300/CBP degradation [1]. When dCBP-1 was applied to the human haploid cell line HAP1 for six hours, CBP and p300 were almost completely lost at doses ranging from 10 to 1000 nM. After one hour of treatment, p300/CBP nearly completely degraded, according to time course analysis using 250 nM dCBP-1 [1].
|
|---|---|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: Multiple myeloma cell line MM1S Tested Concentrations: 10 nM, 100 nM, 250 nM, 500 nM, 1000 nM Incubation Duration: 6 hrs (hours) Experimental Results: demonstrated rapid degradation, p300/CBP after 2 hrs (hours) Almost completely lost. |
| References |
[1]. Raghu Vannam, et al. Targeted degradation of the enhancer lysine acetyltransferases CBP and p300. Cell Chem Biol. 2020 Dec 31;S2451-9456(20)30513-4.
|
| Molecular Formula |
C51H63F2N11O10
|
|---|---|
| Molecular Weight |
1028.1288
|
| Exact Mass |
1027.4727
|
| CAS # |
2484739-25-3
|
| SMILES |
O=C(N1CCC(N(C2CCN(C(CCOCCOCCOCCOCCNC3=CC4=C(C(N(C(CC5)C(NC5=O)=O)C4=O)=O)C=C3)=O)CC2)N=C6N7CCCC8=C7C=C(C(F)F)C(C9=CN(C)N=C9)=C8)=C6C1)NC
|
| Synonyms |
dCBP 1dCBP-1 dCBP1
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~50 mg/mL (~48.63 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (4.86 mM) 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; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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. Solubility in Formulation 2: ≥ 2.86 mg/mL (2.78 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 28.6 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9726 mL | 4.8632 mL | 9.7264 mL | |
| 5 mM | 0.1945 mL | 0.9726 mL | 1.9453 mL | |
| 10 mM | 0.0973 mL | 0.4863 mL | 0.9726 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA