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Art. -Nr.: HY-116636

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KRCA-0377

KRCA-0377 is an orally active ALK inhibitor with an IC₅₀ of 0.001 μM. KRCA-0377 also inhibits mutant ALK enzyme with IC50 values ≤0.01 μM. KRCA-0377 shows cytotoxicity against cancer cells and inhibits tumor growth in xenograft mice models. KRCA-0377 can be used for the research of ALK-positive non-small-cell lung cancer.

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CAS. Nr.: 1845711-03-6
Formel: C₂₃H₂₆ClN₅O₃S
Molecular Weight:488.00

Speicherung:

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

KRCA-0377 Chemical Structure

CAS. Nr.: 1845711-03-6

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

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

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H2228	CC₅₀	0.01 μM Compound: 8	Cytotoxicity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay Cytotoxicity against human NCI-H2228 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay	[PMID: 26712094]
NCI-H3122	CC₅₀	0.008 μM Compound: 8	Cytotoxicity against human NCI-H3122 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay Cytotoxicity against human NCI-H3122 cells assessed as reduction in cell viability measured after 72 hrs by SRB assay	[PMID: 26712094]

In Vitro

KRCA-0377 (Compound 8) (30 min) potently inhibits wild-type ALK with an IC₅₀ of 0.001 μM and ALK^L1196M mutant enzyme with an IC₅₀ of 0.01 μM^[1].
KRCA-0377 (30 min) potently inhibits multiple Crizotinib (HY-50878)-resistant ALK mutant enzymes, including ALK^G1202R (IC₅₀ = 0.0059 μM), ALK^G1269A (IC₅₀ = 0.0017 μM), ALK^{T1151-L1152 inst T} (IC₅₀ = 0.0023 μM), ALK^F1174L (IC₅₀ = 0.0021 μM), and ALK^C1156Y (IC₅₀ = 0.0030 μM)^[1].
KRCA-0377 (72 h) induces cytotoxicity in ALK-positive H2228 (CC₅₀ = 0.01 μM), H3122 (CC₅₀ = 0.008 μM), and Ba/F3 ALK^L1196M (CC₅₀ = 0.036 μM) cells after 72 h of incubation^[1].
KRCA-0377 (1 μM) inhibits approximately one-third of a panel of 96 kinases by over 90%^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

H2228, H3122, Ba/F3 L1196M cells (all harboring EML4-ALK fusion genes)
Concentration:

/
Incubation Time:

72 h
Result:

Induced cytotoxicity in H2228 cells with a CC50 of 0.01 μM.
Induced cytotoxicity in H3122 cells with a CC50 of 0.008 μM.
Induced cytotoxicity in Ba/F3 L1196M cells with a CC50 of 0.036 μM.

Parmacokinetics

Species	Dose	Route	C_max	AUC
Rat^[1]	20 mg/kg	p.o.	1.120 μg/mL	15.900 μg·h/mL

In Vivo

KRCA-0377 (Compound 8) (50 mg/kg; p.o.; daily; 14 days) produces statistically significant inhibition of H3122 xenograft tumor growth in female nude mice^[1].

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

Animal Model:

nude mice with H3122 xenograft (female)^[1]
Dosage:

50 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Achieved significant tumor growth inhibition, with tumor volumes remaining suppressed near the initial ~200 mm³ over the 14-day treatment and observation period.
Demonstrated statistically significant efficacy relative to the control group on the final study day (p < 0.01).
Caused no significant body weight changes in treated mice.

Chemical Information

CAS. Nr. 1845711-03-6
Molecular Weight 488.00
Formel C₂₃H₂₆ClN₅O₃S
SMILES

O=S(=O)(C=1C=CC=CC1NC2=NC(=NC=C2Cl)NC=3C=C4C(=CC3OC)CNCC4)C(C)C
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

Handling Instructions (2659 KB)

Verweise

[1]. Achary R, et al. Discovery of novel tetrahydroisoquinoline-containing pyrimidines as ALK inhibitors. Bioorg Med Chem. 2016;24(2):207-219. [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.

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MOQ

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100 mg

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