Art. -Nr.: HY-144841

Cemsidomide

(Synonyms: CFT7455)

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Cemsidomide (CFT7455) is a ubiquitin ligase pathway based IKZF1/3 (Ikaros/Aiolos) degrader with molecular glue activity. Cemsidomide has a GI₅₀ of 0.05 nM for NCIH929.1 cells. Cemsidomide is used in the research of multiple myeloma (MM).

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Reinheit: 99.54%
CAS. Nr.: 2504235-67-8
Formel: C₂₈H₂₇N₃O₄
Molecular Weight:469.53

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Cemsidomide Chemical Structure

CAS. Nr.: 2504235-67-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cemsidomide (CFT7455) is a ubiquitin ligase pathway based IKZF1/3 (Ikaros/Aiolos) degrader with molecular glue activity^[1]. Cemsidomide has a GI₅₀ of 0.05 nM for NCIH929.1 cells. Cemsidomide is used in the research of multiple myeloma (MM)^[1]^[2].

IC₅₀ & Target^[1]

Cereblon

0.9 nM (Kd)

IKZF1

IKZF3

Alle IKZF Family Isoform-spezifische Produkte anzeigen :

In Vitro

Cemsidomide (0.3 nM; 1.5 h) promotes the degradation of >75% of IKZF1 in multiple myeloma cells. CFT7455 enables potent cell growth inhibition in both previously untreated NCIH929 multiple myeloma cell lines (IC₅₀ of 0.071 nM) and NCIH929 cells made resistant to both Lenalidomide (HY-A0003)/Pomalidomide (HY-10984) (IC₅₀ of 2.3 nM)^[1].
Cemsidomide has potent antiproliferative activity against multiple myeloma cells and IMiD-resistant H929 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In mouse xenograft tumor models, Cemsidomide demonstrates dose dependent efficacy from 3 μg/kg/day to 100 μg/kg/day. In several tumor xenografts tested daily dosing of Cemsidomide at dose of 30 μg/kg/day to 100 μg/kg/day led to durable tumor regression^[1].
Cemsidomide (0.1 mg/kg/day; for 21 days) promotes tumor regression in the H929 tumor xenograft model (95% tumor growth inhibition by 7 days)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2504235-67-8
Appearance Solid
Molecular Weight 469.53
Formel C₂₈H₂₇N₃O₄
Color Light yellow to green yellow
SMILES

O=C1N([C@]2([H])C(NC(CC2)=O)=O)C3=CC=C(C4=CC=CC1=C43)CC5=CC=C(C=C5)CN6CCOCC6
Synonyms

CFT7455
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 66.67 mg/mL (141.99 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. David Proia, et al. Advantageous therapies for disorders mediated by ikaros or aiolos. WO2022032132A1.

[2]. James A. Henderson, et al. Abstract LB007: CFT7455: A novel, IKZF1/3 degrader that demonstrates potent tumor regression in IMiD-resistant multiple myeloma (MM) xenograft models. Cancer Res (2021) 81 (13_Supplement): LB007.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1298 mL	10.6489 mL	21.2979 mL	53.2447 mL
	5 mM	0.4260 mL	2.1298 mL	4.2596 mL	10.6489 mL
	10 mM	0.2130 mL	1.0649 mL	2.1298 mL	5.3245 mL
	15 mM	0.1420 mL	0.7099 mL	1.4199 mL	3.5496 mL
	20 mM	0.1065 mL	0.5324 mL	1.0649 mL	2.6622 mL
	25 mM	0.0852 mL	0.4260 mL	0.8519 mL	2.1298 mL
	30 mM	0.0710 mL	0.3550 mL	0.7099 mL	1.7748 mL
	40 mM	0.0532 mL	0.2662 mL	0.5324 mL	1.3311 mL
	50 mM	0.0426 mL	0.2130 mL	0.4260 mL	1.0649 mL
	60 mM	0.0355 mL	0.1775 mL	0.3550 mL	0.8874 mL
	80 mM	0.0266 mL	0.1331 mL	0.2662 mL	0.6656 mL
	100 mM	0.0213 mL	0.1065 mL	0.2130 mL	0.5324 mL

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Cemsidomide

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Molecular Glue Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Molecular Glue-like Compound Library

Alle IKZF Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cemsidomide

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Molecular Glue Compound Library

Heterocyclic Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Molecular Glue-like Compound Library

Alle IKZF Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cemsidomide Related Classifications

HY-144841 Related Classifications