Art. -Nr.: HY-159646

BMS-986397

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BMS-986397 is a potent, selective, and orally active cereblon-based molecular glue degrader of casein kinase 1α (CK1α). BMS-986397 induces apoptosis and cell cycle arrest in acute myeloid leukemia (AML) cells. BMS-986397 is a promising agent for the investigation of AML and high-risk myelodysplastic syndromes (HR-MDS).

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Reinheit: 99.76%
CAS. Nr.: 2564486-44-6
Formel: C₂₁H₁₆ClF₃N₄O₄
Molecular Weight:480.82

Speicherung:

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

BMS-986397 Chemical Structure

CAS. Nr.: 2564486-44-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Cereblon

Alle Ligands for E3 Ligase Isoform-spezifische Produkte anzeigen :

Alle Casein Kinase Isoform-spezifische Produkte anzeigen :

In Vitro

BMS‑986397 demonstrates significant anti‑proliferative activity in TP53 wild‑type AML cell lines via potent and selective degradation of CK1α. Degradation of CK1α leads to stabilization of p53 protein and upregulation of its downstream transcriptional targets, including p21, PUMA and BAX, thereby inducing cell cycle arrest and acute apoptosis in AML cells^[2].

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

Chemical Information

CAS. Nr. 2564486-44-6
Appearance Solid
Molecular Weight 480.82
Formel C₂₁H₁₆ClF₃N₄O₄
Color White to off-white
SMILES

O=C1CC[C@@H](C(N1)=O)N2CC3=C(C2=O)C=CC(C(N[C@@H](C(F)(F)F)C4=NC=CC=C4Cl)=O)=C3
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 : 100 mg/mL (207.98 mM; Need ultrasonic; 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

2.0798 mL

10.3989 mL

20.7978 mL

5 mM

0.4160 mL

2.0798 mL

4.1596 mL

10 mM

0.2080 mL

1.0399 mL

2.0798 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: ≥ 5 mg/mL (10.40 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

Solubility: ≥ 5 mg/mL (10.40 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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 (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Carmen Jimenez, et al. BMS-986397, a First-in-Class Molecular Glue Degrader of Casein Kinase 1α (CK1α) for the Treatment of Acute Myeloid Leukemia (AML) and High-Risk Myelodysplastic Syndrome (HR-MDS) Harboring Functional TP53. Blood. Volume 144, Supplement 1, 5 November 2024, Page 4142.

[2]. Jimenez C, et al. BMS-986397, a First-in-Class Molecular Glue Degrader of Casein Kinase 1α (CK1α) for the Treatment of Acute Myeloid Leukemia (AML) and High-Risk Myelodysplastic Syndrome (HR-MDS) Harboring Functional TP53. Blood, 2024, 144: 4142.

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	2.0798 mL	10.3989 mL	20.7978 mL	51.9945 mL
	5 mM	0.4160 mL	2.0798 mL	4.1596 mL	10.3989 mL
	10 mM	0.2080 mL	1.0399 mL	2.0798 mL	5.1995 mL
	15 mM	0.1387 mL	0.6933 mL	1.3865 mL	3.4663 mL
	20 mM	0.1040 mL	0.5199 mL	1.0399 mL	2.5997 mL
	25 mM	0.0832 mL	0.4160 mL	0.8319 mL	2.0798 mL
	30 mM	0.0693 mL	0.3466 mL	0.6933 mL	1.7332 mL
	40 mM	0.0520 mL	0.2600 mL	0.5199 mL	1.2999 mL
	50 mM	0.0416 mL	0.2080 mL	0.4160 mL	1.0399 mL
	60 mM	0.0347 mL	0.1733 mL	0.3466 mL	0.8666 mL
	80 mM	0.0260 mL	0.1300 mL	0.2600 mL	0.6499 mL
	100 mM	0.0208 mL	0.1040 mL	0.2080 mL	0.5199 mL

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BMS-986397

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Anti-Cardiovascular Disease Compound Library

Ubiquitination Compound Library

Ferroptosis Compound Library

Pyroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

E3 Ligase Ligand Library

Cancer Stem Cells Compound Library

Molecular Glue Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Alle Ligands for E3 Ligase Isoform-spezifische Produkte anzeigen

Alle Casein Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BMS-986397 Related Classifications

HY-159646 Related Classifications