Referencia número: HY-144288

BLK-IN-2

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Based on 1 Customer Validation

BLK-IN-2 (compound 25) is a potent and selective irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), with an IC₅₀ of 5.9 nM. BLK-IN-2 also inhibits BTK (IC₅₀=202.0 nM). BLK-IN-2 shows potent antiproliferative activities against several lymphoma cells.

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Pureza: 98.61%
No. CAS: 2694871-86-6
Fòrmula: C₃₉H₄₁N₉O₃
Peso molecular:683.80

Almacenamiento:

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

BLK-IN-2 Chemical Structure

No. CAS: 2694871-86-6

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Amount: USD 0.00

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

IC50: 5.9 nM (BLK)^[1], 202.0 nM (BTK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	GI₅₀	>30 μM Compound: 25	Antiproliferative activity against human A-375 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human A-375 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
A-431	GI₅₀	>30 μM Compound: 25	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
A549	GI₅₀	>30 μM Compound: 25	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
DOHH-2	GI₅₀	0.016 μM Compound: 25	Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
HBL1	GI₅₀	1.34 μM Compound: 25	Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
HCT-116	GI₅₀	8.1 μM Compound: 25	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
HEK293	GI₅₀	>30 μM Compound: 25	Antiproliferative activity against HEK293 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against HEK293 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
Jurkat	GI₅₀	10.9 μM Compound: 25	Antiproliferative activity against human Jurkat cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human Jurkat cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
MDA-MB-453	GI₅₀	>30 μM Compound: 25	Antiproliferative activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
MOLT-4	GI₅₀	18.8 μM Compound: 25	Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
OCI-Ly7	GI₅₀	0.02 μM Compound: 25	Antiproliferative activity against human OCILY7 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human OCILY7 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
PBMC	GI₅₀	>30 μM Compound: 25	Antiproliferative activity against human PBMC cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human PBMC cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
Pfeiffer	GI₅₀	2.18 μM Compound: 25	Antiproliferative activity against human Pfeiffer cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human Pfeiffer cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
SU-DHL10	GI₅₀	0.56 μM Compound: 25	Antiproliferative activity against human SU-DHL-10 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human SU-DHL-10 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
SU-DHL-6	GI₅₀	0.13 μM Compound: 25	Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]
TMD8	GI₅₀	0.064 μM Compound: 25	Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 34952433]

Chemical Information

No. CAS 2694871-86-6
Appearance Solid
Peso molecular 683.80
Fòrmula C₃₉H₄₁N₉O₃
Color Light yellow to yellow
SMILES

O=C(C1=CC2=C(C=NC=C2)C=C1)NC3=CC=C(C)C(C(NC4=CN=C(NC5=CC=CC(NC6CCN(C(/C=C/CN(C)C)=O)CC6)=C5)N=C4)=O)=C3
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (146.24 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

1.4624 mL

7.3121 mL

14.6242 mL

5 mM

0.2925 mL

1.4624 mL

2.9248 mL

10 mM

0.1462 mL

0.7312 mL

1.4624 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.08 mg/mL (3.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (267 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Fu T, et, al. Discovery of selective irreversible inhibitors of B-Lymphoid tyrosine kinase (BLK). Eur J Med Chem. 2022 Feb 5;229:114051. [Content Brief]

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	1.4624 mL	7.3121 mL	14.6242 mL	36.5604 mL
	5 mM	0.2925 mL	1.4624 mL	2.9248 mL	7.3121 mL
	10 mM	0.1462 mL	0.7312 mL	1.4624 mL	3.6560 mL
	15 mM	0.0975 mL	0.4875 mL	0.9749 mL	2.4374 mL
	20 mM	0.0731 mL	0.3656 mL	0.7312 mL	1.8280 mL
	25 mM	0.0585 mL	0.2925 mL	0.5850 mL	1.4624 mL
	30 mM	0.0487 mL	0.2437 mL	0.4875 mL	1.2187 mL
	40 mM	0.0366 mL	0.1828 mL	0.3656 mL	0.9140 mL
	50 mM	0.0292 mL	0.1462 mL	0.2925 mL	0.7312 mL
	60 mM	0.0244 mL	0.1219 mL	0.2437 mL	0.6093 mL
	80 mM	0.0183 mL	0.0914 mL	0.1828 mL	0.4570 mL
	100 mM	0.0146 mL	0.0731 mL	0.1462 mL	0.3656 mL

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BLK-IN-2

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

BLK-IN-2

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

BLK-IN-2 Related Classifications

HY-144288 Related Classifications