Art. -Nr.: HY-121495

BKI-1369

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BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC₅₀ of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves.

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Reinheit: 99.37%
CAS. Nr.: 1951431-22-3
Formel: C₂₃H₂₇N₇O
Molecular Weight:417.51

Speicherung:

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

BKI-1369 Chemical Structure

CAS. Nr.: 1951431-22-3

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 1.52 μM (hERG)^[1]

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Cellular Effect

Cell Line	Type	Value	Description	References
CAPAN-1	IC₅₀	>100 μM Compound: BKI1369	Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis	[PMID: 32835918]
HCT-116	IC₅₀	>55.2 μM Compound: BKI1369	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis	[PMID: 32835918]
HepG2	GI₅₀	>10 μM Compound: 17	Growth inhibition of human HepG2 cells after 48 hrs by Alamar blue assay Growth inhibition of human HepG2 cells after 48 hrs by Alamar blue assay	[PMID: 27309760]
HL-60	IC₅₀	>100 μM Compound: BKI1369	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis	[PMID: 32835918]
K562	IC₅₀	>100 μM Compound: BKI1369	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis	[PMID: 32835918]
LN-229	IC₅₀	45.2 μM Compound: BKI1369	Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis	[PMID: 32835918]
NCI-H460	IC₅₀	>100 μM Compound: BKI1369	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis	[PMID: 32835918]
Z-138	IC₅₀	30.4 μM Compound: BKI1369	Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis	[PMID: 32835918]

Chemical Information

CAS. Nr. 1951431-22-3
Appearance Solid
Molecular Weight 417.51
Formel C₂₃H₂₇N₇O
Color White to off-white
SMILES

NC1=C2C(N(CC3CCN(C)CC3)N=C2C4=CC=C5N=C(OCC)C=CC5=C4)=NC=N1
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 : 50 mg/mL (119.76 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

2.3952 mL

11.9758 mL

23.9515 mL

5 mM

0.4790 mL

2.3952 mL

4.7903 mL

10 mM

0.2395 mL

1.1976 mL

2.3952 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 (11.98 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 (11.98 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 (272 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]. Lee S, et al. Therapeutic Efficacy of Bumped Kinase Inhibitor 1369 in a Pig Model of Acute Diarrhea Caused by Cryptosporidium hominis. Antimicrob Agents Chemother. 2018 Jun 26;62(7). [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	2.3952 mL	11.9758 mL	23.9515 mL	59.8788 mL
	5 mM	0.4790 mL	2.3952 mL	4.7903 mL	11.9758 mL
	10 mM	0.2395 mL	1.1976 mL	2.3952 mL	5.9879 mL
	15 mM	0.1597 mL	0.7984 mL	1.5968 mL	3.9919 mL
	20 mM	0.1198 mL	0.5988 mL	1.1976 mL	2.9939 mL
	25 mM	0.0958 mL	0.4790 mL	0.9581 mL	2.3952 mL
	30 mM	0.0798 mL	0.3992 mL	0.7984 mL	1.9960 mL
	40 mM	0.0599 mL	0.2994 mL	0.5988 mL	1.4970 mL
	50 mM	0.0479 mL	0.2395 mL	0.4790 mL	1.1976 mL
	60 mM	0.0399 mL	0.1996 mL	0.3992 mL	0.9980 mL
	80 mM	0.0299 mL	0.1497 mL	0.2994 mL	0.7485 mL
	100 mM	0.0240 mL	0.1198 mL	0.2395 mL	0.5988 mL

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BKI-1369

MCE Bioactive Compound Library

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BKI-1369 Related Classifications

HY-121495 Related Classifications