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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- No. CAS: 1845711-03-6
- Fòrmula: C23H26ClN5O3S
- Peso molecular:488.00
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H2228 | CC50 |
0.01 μM
Compound: 8
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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
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[PMID: 26712094] |
| NCI-H3122 | CC50 |
0.008 μM
Compound: 8
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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
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[PMID: 26712094] |
KRCA-0377 (Compound 8) (30 min) potently inhibits wild-type ALK with an IC50 of 0.001 μM and ALKL1196M 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 ALKG1202R (IC50 = 0.0059 μM), ALKG1269A (IC50 = 0.0017 μM), ALKT1151-L1152 inst T (IC50 = 0.0023 μM), ALKF1174L (IC50 = 0.0021 μM), and ALKC1156Y (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 ALKL1196M (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.
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Cell Line:H2228, H3122, Ba/F3 L1196M cells (all harboring EML4-ALK fusion genes)
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Concentration:/
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Incubation Time:72 h
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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.
| Species | Dose | Route | Cmax | AUC |
|---|---|---|---|---|
| Rat[1] | 20 mg/kg | p.o. | 1.120 μg/mL | 15.900 μg·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nude mice with H3122 xenograft (female)[1]
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Dosage:50 mg/kg
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Administration:p.o.; daily; 14 days
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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
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No. CAS 1845711-03-6
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Peso molecular 488.00
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Fòrmula C23H26ClN5O3S
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SMILES
O=S(=O)(C=1C=CC=CC1NC2=NC(=NC=C2Cl)NC=3C=C4C(=CC3OC)CNCC4)C(C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KRCA-0377 Related Classifications
HY-116636 Related Classifications
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- KRCA-0377
- 1845711-03-6
- KRCA0377
- KRCA 0377
- Anaplastic lymphoma kinase (ALK)
- ALK kinase activity
- antineoplastic agent
- xenograft models
- ALK L1196M mutant enzyme
- G1202R ALK mutant
- T1151-L1152 inst T ALK mutant enzyme
- F1174L ALK mutant enzyme
- wild-type ALK
- G1269A ALK mutant enzyme
- ALK-positive non-small-cell lung cancer
- Inhibitor
- inhibitor
- inhibit