| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| Other Sizes |
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| ln Vitro |
In multiple myeloma cells, cemsidomide stimulates the degradation of >75% of steady-state IKZF1 in 1.5 hours at 0.3 nM. Both NCIH929 cells resistant to both lenalidomide and pomalidomide (IC50 of 2.3 nM) and previously untreated NCIH929 multiple myeloma cell lines (IC50 of 0.071 nM) are efficiently inhibited by the strong binding affinity and degradation catalysis of CFT7455 [1]. When applied to IMiD-resistant H929 cells and multiple myeloma cells, cemsidomide exhibits strong antiproliferative action [2].
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| ln Vivo |
Cemsidomide showed dose-dependent effectiveness in mice xenograft tumor models, with doses ranging from 3 μg/kg/day to 100 μg/kg/day. In many tumor xenograft experiments, cemsidomide administered daily at doses ranging from 30 μg/kg/day to 100 μg/kg/day produced long-lasting tumor regression [1]. In a H929 tumor xenograft model, cemsidomide (0.1 mg/kg/day; for 21 days) promotes tumor regression (95% tumor growth suppression at 7 days) [2].
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| References | |
| Additional Infomation |
Cemsidomide is an orally bioavailable modulator of the E3 ubiquitin ligase complex containing cereblon (CRL4-CRBN E3 ubiquitin ligase), with potential immunomodulating and antineoplastic activities. Upon oral administration, cemsidomide specifically binds to cereblon (CRBN), thereby affecting the ubiquitin E3 ligase activity, and targeting certain substrate proteins for ubiquitination. This induces proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3), which are transcriptional repressors in T-cells. This reduces the levels of these transcription factors, and modulates the activity of the immune system, which may include the activation of T-lymphocytes. This also leads to downregulation of the activity of other proteins, some of which play key roles in the proliferation of certain cancer cell types. CRBN, the substrate recognition component of the CRL4-CRBN E3 ubiquitin ligase complex, plays a key role in the ubiquitination of certain proteins.
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| Molecular Formula |
C28H27N3O4
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|---|---|
| Molecular Weight |
469.53
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| Exact Mass |
469.2
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| CAS # |
2504235-67-8
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| PubChem CID |
155207651
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| Appearance |
Light yellow to green yellow solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
819
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C1[C@@H](N2C(=O)C3=C4C(C(CC5=CC=C(C=C5)CN5CCOCC5)=CC=C24)=CC=C3)CCC(=O)N1
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| InChi Key |
MUKCJOOKCZSQNW-DEOSSOPVSA-N
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| InChi Code |
InChI=1S/C28H27N3O4/c32-25-11-10-24(27(33)29-25)31-23-9-8-20(21-2-1-3-22(26(21)23)28(31)34)16-18-4-6-19(7-5-18)17-30-12-14-35-15-13-30/h1-9,24H,10-17H2,(H,29,32,33)/t24-/m0/s1
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| Chemical Name |
(3S)-3-[6-[[4-(morpholin-4-ylmethyl)phenyl]methyl]-2-oxobenzo[cd]indol-1-yl]piperidine-2,6-dione
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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 : ~25 mg/mL (~53.24 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.32 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 25.0 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: ≥ 2.5 mg/mL (5.32 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1298 mL | 10.6489 mL | 21.2979 mL | |
| 5 mM | 0.4260 mL | 2.1298 mL | 4.2596 mL | |
| 10 mM | 0.2130 mL | 1.0649 mL | 2.1298 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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