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Art. -Nr.: HY-108230

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ALK-IN-12

ALK-IN-12 is a potent and orally active ALK inhibitor with an IC₅₀ of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC₅₀=20.3 and 90.6 nM). Antitumor activities.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1197958-53-4
Formel: C₂₄H₃₀ClN₆O₂P
Molecular Weight:500.96

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

ALK-IN-12 Chemical Structure

CAS. Nr.: 1197958-53-4

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Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

ALK-IN-12 is a potent and orally active ALK inhibitor with an IC₅₀ of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC₅₀=20.3 and 90.6 nM). Antitumor activities^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
KARPAS-299	IC₅₀	28.3 nM Compound: 11e	Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]
U-937	IC₅₀	1590 nM Compound: 11e	Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 27144831]

In Vitro

ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC₅₀ of 28.3 nM^[1].

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

In Vivo

ALK-IN-12 (10-50 mg/kg; orally; once daily for 13 consecutive days) shows dose-dependent antitumor activity^[1].
ALK-IN-12 (3 mg/kg; i.v.; 6-8 week old female CD rats ) treatment shows AUC_0-∞, CL, t_1/2 and V_ss are 3039 ng h/mL, 0.91 h kg, 6.6 hours and 6.12 L/kg, respectively^[1].
ALK-IN-12 (10 mg/kg; p.o.; 6-8 week old female CD rats) treatment shows C_max, AUC_0-∞, t_max, t_1/2 and F are 3254 ng/mL, 4056 ng h/mL, 6.0 hours, 12.5 hours and 39%, respectively^[1].

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

Animal Model:

Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)^[1]
Dosage:

10-50 mg/kg
Administration:

Orally; once daily for 13 consecutive days
Result:

Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose).

Chemical Information

CAS. Nr. 1197958-53-4
Molecular Weight 500.96
Formel C₂₄H₃₀ClN₆O₂P
SMILES

CN1CCN(C2=CC=C(NC3=NC=C(Cl)C(NC4=CC=CC=C4P(C)(C)=O)=N3)C(OC)=C2)CC1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 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]. Huang WS, et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem. 2016;59(10):4948-4964. [Content Brief]

Calculators

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)}

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.

Keywords

MOQ

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100 mg

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