Art. -Nr.: HY-147259

Dalmelitinib

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Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC₅₀: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC).

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Reinheit: 98.65%
CAS. Nr.: 1637658-98-0
Formel: C₂₂H₁₆FN₇O₂S
Molecular Weight:461.47

Speicherung:

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

Dalmelitinib Chemical Structure

CAS. Nr.: 1637658-98-0

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

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>10000 nM Compound: 4d	Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human A549 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
HCCLM3	IC₅₀	33 nM Compound: 4d	Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human HCCLM3 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
Huh-7	IC₅₀	>10000 nM Compound: 4d	Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human HuH7 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
MHCC97H	IC₅₀	6 nM Compound: 4d	Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human MHCC97H cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
MKN-45	IC₅₀	6 nM Compound: 4d	Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human MKN45 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
NCI-H1975	IC₅₀	>10000 nM Compound: 4d	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
NCI-H1993	IC₅₀	14 nM Compound: 4d	Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human NCI-H1993 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
NCI-N87	IC₅₀	>10000 nM Compound: 4d	Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human NCI-N87 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]
SNU-5	IC₅₀	2 nM Compound: 4d	Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay Cytotoxicity against human SNU5 cells assessed as reduction in cell survival incubated for 3 days by cell titre-glo assay	[PMID: 27288183]

In Vitro

Dalmelitinib (Compound 4 d) binds to the ATP-binding region of c-Met kinase, and shows slective inhibitory activity against c-Met with an IC₅₀ value of 2.9 nM^[1].
Dalmelitinib (0-1 μM approximately, 3 days) inhibits cell proliferation in various c-Met oncogene amplification cancer cell lines, with IC₅₀ values ranging from 6 nM to 33 nM^[1].
Dalmelitinib (0.1-1 μM, 6-24 h) significantly induces the phosphorylation of the tyrosine kinases (MET), partially or completely inhibits the downstream phosphorylation of ERK and AKT in HCCLM3 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

C-Met oncogene amplification cancer cell: SNU-5, HCCLM3, MHCC97-H, MHCC97-L, MKN-45, NCI-H1993.
No C-Met oncogene amplification cancer cell: Huh-7, NCI-N87, NCI-1975, A549.
Concentration:

0-1 μM approximately.
Incubation Time:

3 days
Result:

IC₅₀: 33 nM (HCCLM3), 6 nM (MHCC97-H, MKN-45), 7 nM (MHCC97-L), 14 nM (NCI-H1993), 2 nM (SNU-5); Other cells: > 1000 nM.

Western Blot Analysis^[1]

Cell Line:

C-Met oncogene amplification cancer cell: SNU-5, HCCLM3, MHCC97-H, MHCC97-L, MKN-45, NCI-H1993.
No C-Met oncogene amplification cancer cell: Huh-7, NCI-N87, NCI-1975, A549.
Concentration:

0.1, 0.3, 1 μM
Incubation Time:

6-24 h
Result:

Significantly induced the phosphorylation of the tyrosine kinases (MET), partially inhibited the downstream phosphorylation of AKT, and completely inhibited the downstream phosphorylation of ERK.

In Vivo

Dalmelitinib (Compound 4 d, intragastric administration, 10-60 mg/kg) significantly inhibits the tumor growth in a dose-dependent manner in MKN-45 tumor xenograft nude mice^[1].
Dalmelitinib (intragastric administration, 5 mg/kg for a single dose) shows a high plasma concentration, longer half-life and mean residence time, low clearance rates in BALB/c small nude mice^[1].
Dalmelitinib shows a high level of No Observed Adverse Effect Level (NOAEL) in mice long-term toxicity (225 mg/kg/day) and acute toxicity (600 mg/kg/day)^[1].

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

Animal Model:

MKN-45 tumor xenograft nude mice^[1]
Dosage:

10, 30, 60 mg/kg
Administration:

Intragastric administration
Result:

Inhibited the tumor growth with the inhibitory rates of 29.5% (10 mg/kg), 34.2% (30 mg/kg), and 61.4% (60 mg/kg).

Animal Model:

BALB/c small nude mice (pharmacokinetic assay)^[1]
Dosage:

5 mg/kg for a single dose
Administration:

Intragastric administration
Result:

Pharmacokinetic profile of Dalmelitinib (Compound 4 d)

Compound Cmax (ng/mL) AUC (ng/mL/h) t_1/2 (h) MRT (h) CL/F (mL/min/kg) Vz/F

Dalmelitinib 8628 122487 5.55 9.10 0.68 327

Chemical Information

CAS. Nr. 1637658-98-0
Appearance Solid
Molecular Weight 461.47
Formel C₂₂H₁₆FN₇O₂S
Color White to off-white
SMILES

O=C1N(C)C2=CN=C3C=CC(SC4=NN=C5C(F)=CC(C6=CN(C)N=C6)=CN45)=CC3=C2OC1
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 (216.70 mM; ultrasonic and warming and heat to 80°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

2.1670 mL

10.8349 mL

21.6699 mL

5 mM

0.4334 mL

2.1670 mL

4.3340 mL

10 mM

0.2167 mL

1.0835 mL

2.1670 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 (5.42 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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% Corn Oil

Solubility: 2.5 mg/mL (5.42 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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 (280 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]. Junjun Zhao, et al. Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors. Bioorg Med Chem. 2016 Aug 15;24(16):3483-93. [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	2.1670 mL	10.8349 mL	21.6699 mL	54.1747 mL
	5 mM	0.4334 mL	2.1670 mL	4.3340 mL	10.8349 mL
	10 mM	0.2167 mL	1.0835 mL	2.1670 mL	5.4175 mL
	15 mM	0.1445 mL	0.7223 mL	1.4447 mL	3.6116 mL
	20 mM	0.1083 mL	0.5417 mL	1.0835 mL	2.7087 mL
	25 mM	0.0867 mL	0.4334 mL	0.8668 mL	2.1670 mL
	30 mM	0.0722 mL	0.3612 mL	0.7223 mL	1.8058 mL
	40 mM	0.0542 mL	0.2709 mL	0.5417 mL	1.3544 mL
	50 mM	0.0433 mL	0.2167 mL	0.4334 mL	1.0835 mL
	60 mM	0.0361 mL	0.1806 mL	0.3612 mL	0.9029 mL
	80 mM	0.0271 mL	0.1354 mL	0.2709 mL	0.6772 mL
	100 mM	0.0217 mL	0.1083 mL	0.2167 mL	0.5417 mL

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Dalmelitinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Compound	Cmax (ng/mL)	AUC (ng/mL/h)	t_1/2 (h)	MRT (h)	CL/F (mL/min/kg)	Vz/F
Dalmelitinib	8628	122487	5.55	9.10	0.68	327

Dalmelitinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Dalmelitinib Related Classifications

HY-147259 Related Classifications