2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK)
  4. 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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KRCA-0377

KRCA-0377 Chemical Structure

CAS No. : 1845711-03-6

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KRCA-0377 Related Antibodies

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Description

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[1].

In Vitro

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.

KRCA-0377 Related Antibodies

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 Cmax 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.
Molecular Weight

488.00

Formula

C23H26ClN5O3S
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KRCA-0377 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KRCA-03771845711-03-6KRCA0377KRCA 0377Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALK kinase activityantineoplastic agentxenograft modelsALK L1196M mutant enzymeG1202R ALK mutantT1151-L1152 inst T ALK mutant enzymeF1174L ALK mutant enzymewild-type ALKG1269A ALK mutant enzymeALK-positive non-small-cell lung cancerInhibitorinhibitorinhibit

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