Art. -Nr.: HY-153857

Lasmotinib

(Synonyms: PHI-101)

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Lasmotinib (PHI-101) is a FLT3 and CHK2 inhibitor. Lasmotinib potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. Lasmotinib synergizes with Venetoclax (HY-15531) or Azacytidine to inhibit leukemia. Lasmotinib exhibits anticancer activity against ovarian and breast cancer.

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Reinheit: 98.16%
CAS. Nr.: 2127107-15-5
Formel: C₁₉H₁₉FN₄O₂S
Molecular Weight:386.44

Speicherung:

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

Lasmotinib Chemical Structure

CAS. Nr.: 2127107-15-5

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Use of MCE Products

Fluorescent Dye

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

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

IC₅₀ & Target^[1]^[2]^[3]^[4]

Chk2

Alle Checkpoint Kinase (Chk) Isoform-spezifische Produkte anzeigen :

In Vitro

Lasmotinib (PHI-101) 是一种 FLT3 和 CHK2 抑制剂。Lasmotinib 有效抑制 FLT3 单激活突变 (ITD 或 TKD 突变体)，并对 FLT3 双 (ITD/D835Y 或 ITD/F691L) 和三 (ITD/D835Y/F691L) 耐药突变具有抑制活性。Lasmotinib 与 Venetoclax (HY-15531) 或 Azacytidine 协同抑制白血病。Lasmotinib 对卵巢癌和乳腺癌表现出抗癌活性^[1]^[2]^[3]^[4]。

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

In Vivo

Lasmotinib 抑制 FLT3 突变细胞 MV4-11、Molm13 和 Molm14 的生长，GI₅₀ 值分别为 7.0 nM、3.8 nM 和 3.4 nM^[2]。
Lasmotinib (72 h) 与 PARP1 抑制剂 Olaparib (HY-10162) 联合治疗卵巢癌细胞和乳腺癌细胞无论细胞中是否存在功能性 BRCA 和 P53 都引发协同致死反应^[3]。
Lasmotinib 对难治性卵巢癌细胞和乳腺癌细胞表现出抗癌活性^[3]。
Lasmotinib 与 Venetoclax (HY-15531) 或 Azacytidine 联合治疗对 FLT3-ITD 突变型和野生型 AML 细胞生长抑制表现出强大的协同作用^[4]。

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. 2127107-15-5
Appearance Solid
Molecular Weight 386.44
Formel C₁₉H₁₉FN₄O₂S
Color White to yellow
SMILES

NC(NC1=C(SC(C#CC2=CC(F)=CC=C2)=C1)C(N[C@H]3CCCNC3)=O)=O
Synonyms

PHI-101
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 (258.77 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

2.5877 mL

12.9386 mL

25.8772 mL

5 mM

0.5175 mL

2.5877 mL

5.1754 mL

10 mM

0.2588 mL

1.2939 mL

2.5877 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 (6.47 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% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.47 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 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 (6.47 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 (275 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]. Nam K Y, et al. PHI-101 Is a Potent Third-Generation FLT3 Inhibitor Developed to Overcome Resistance in Acute Myeloid Leukemia[J]. Blood, 2020, 136: 28.

[2]. Sung G J, Kim K A, Nam K Y, et al. Evaluation of Synergistic Anti-Leukemic Efficacy of PHI-101 in Preclinical Model of FLT3-ITD Acute Myeloid Leukemia. Blood, 2023, 142: 5949.

[3]. Han J H J, Kim K T, Im J, et al. PHI-101, a potent and novel inhibitor of CHK2 in ovarian and breast cancer cells. Cancer Research, 2021, 81(13_Supplement): 1461-1461.

[4]. Hwang H, Sung G J, Kim K A, et al. PHI-101 synergizes with chemotherapy and venetoclax in preclinical models of acute myeloid leukemia. Cancer Research, 2024, 84(6_Supplement): 7153-7153.

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	2.5877 mL	12.9386 mL	25.8772 mL	64.6931 mL
	5 mM	0.5175 mL	2.5877 mL	5.1754 mL	12.9386 mL
	10 mM	0.2588 mL	1.2939 mL	2.5877 mL	6.4693 mL
	15 mM	0.1725 mL	0.8626 mL	1.7251 mL	4.3129 mL
	20 mM	0.1294 mL	0.6469 mL	1.2939 mL	3.2347 mL
	25 mM	0.1035 mL	0.5175 mL	1.0351 mL	2.5877 mL
	30 mM	0.0863 mL	0.4313 mL	0.8626 mL	2.1564 mL
	40 mM	0.0647 mL	0.3235 mL	0.6469 mL	1.6173 mL
	50 mM	0.0518 mL	0.2588 mL	0.5175 mL	1.2939 mL
	60 mM	0.0431 mL	0.2156 mL	0.4313 mL	1.0782 mL
	80 mM	0.0323 mL	0.1617 mL	0.3235 mL	0.8087 mL
	100 mM	0.0259 mL	0.1294 mL	0.2588 mL	0.6469 mL

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Lasmotinib

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Alle Checkpoint Kinase (Chk) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lasmotinib

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Alkyne Compound Library

Alle Checkpoint Kinase (Chk) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lasmotinib Related Classifications

HY-153857 Related Classifications