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  3. Taletrectinib free base

Taletrectinib free base  (Synonyms: DS-6051b free base; AB-106 free base; IBI-344 free base)

Cat. No.: HY-131003A
Handling Instructions

Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.

For research use only. We do not sell to patients.

Taletrectinib free base Chemical Structure

Taletrectinib free base Chemical Structure

CAS No. : 1505514-27-1

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Description

Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants[1][2].

In Vitro

The IC50 of Taletrectinib free base (1-1000 nM; 72 hours) against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, or KM12 cells is ~3-20 nM[1].
Taletrectinib free base (0.001-1000 nM; 2 hours) dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells in vitro[1].
Taletrectinib (DS-6051b) free base potently inhibits autophosphorylation of ROS1 in JFCR-165, JFCR-168, and MGH193-1B cells[1].
Taletrectinib free base partially suppresses phospho-NTRK1 at 10 nM, and completely suppresses by 100 nM. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in an ATP-competitive manner. Taletrectinib free base almost completely inhibits ACK, ALK, DDR1, and LTK at 0.2 μM among 160 kinases in the presence of 1 mM ATP, but did not inhibit other 152 kinases strongly[1].
Taletrectinib free base effectively inhibits Crizotinib-resistant ROS1 secondary mutations, including G2032R solvent front mutation[1].

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

Cell Viability Assay[1]

Cell Line: TPM3-NTRK1-induced Ba/F3 cells, KM12 cells
Concentration: 1-1000 nM
Incubation Time: 72 hours
Result: Inhibited TPM3-NTRK1-induced Ba/F3 cells and KM12 cells viability.

Western Blot Analysis[1]

Cell Line: U-118 MG cells (harboring FIG-ROS1 fusion gene)
Concentration: 0.001-1000 nM
Incubation Time: 2 hours
Result: Dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells.
In Vivo

Taletrectinib (DS-6051b) free base (25-200 mg/kg; p.o.; once daily for 18 days) shows antitumor activity[1].
Taletrectinib free base (6.25-200 mg/kg; p.o.; once daily for 8 days) inhibits NTRK-rearranged cancer in Balb-c nu/nu mice bearing KM12 cells[1].
Taletrectinib free base (3-100 mg/kg; p.o.; once daily for 4 days) shows rapid tumor regression in the wild-type (WT) and the G2032R-mutant Ba/F3-bearing mice without severe body weight loss[1].

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

Animal Model: Balb-c nu/nu mice (bearing U-118 MG cells)[1]
Dosage: 25, 50, 100, and 200 mg/kg
Administration: P.o.; once daily for 18 days
Result: Effectively inhibited tumor growth at ≥25 mg/kg without significant body weight loss.
Clinical Trial
Molecular Weight

405.47

Formula

C23H24FN5O

CAS No.
SMILES

C[C@@H](NC1=NN2C(C=C1)=NC=C2C3=CC=C(OC[C@H](N)C)C=C3)C4=CC=CC(F)=C4

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
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Taletrectinib free base 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.

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