An ROS1, TrkA, and TrkC inhibitor
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Taletrectinib

Item No. 45040

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[4-[(2R)-2-aminopropoxy] phenyl]-N-[(1R)-1-(3-fluorophenyl)ethyl]-Imidazo[1,2-b]pyridazin-6-amine
CAS Number
1505514-27-1
Synonyms
  • AB-106
  • DS-6051b
Molecular Formula
C23H24FN5O
Formula Weight
405.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
C[C@@H](N)COC1=CC=C(C2=CN=C3C=CC(N[C@H](C)C4=CC(F)=CC=C4)=NN32)C=C1
InChi Code
InChI=1S/C23H24FN5O/c1-15(25)14-30-20-8-6-17(7-9-20)21-13-26-23-11-10-22(28-29(21)23)27-16(2)18-4-3-5-19(24)12-18/h3-13,15-16H,14,25H2,1-2H3,(H,27,28)/t15-,16-/m1/s1
InChi Key
HEVHTYMYEMEBPX-HZPDHXFCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $735

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    Product Description

    Taletrectinib is an inhibitor of c-Ros oncogene 1 (ROS1), tropomyosin-related kinase A (TrkA), and TrkC (IC50s = 0.207, 0.622, and 0.98 nM, respectively).1 It is selective for these kinases over TrkB (IC50 = 2.28 nM). Talectrectinib (1-10,000 nM) reduces the viability of JFCR-165, JFCR-168, and MGH193-1B patient-derived CD74-ROS1 fusion protein-positive non-small cell lung cancer (NSCLC) cells. In vivo, talectrectinib (25-100 mg/kg) reduces tumor volume in Ba/F3 mouse xenograft models expressing CD74-ROS1 wild-type fusion proteins or crizotinib-resistant CD74-ROS1G2032R mutant fusion proteins.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Katayama, R., Gong, B., Togashi, N., et al. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat. Commun. 10(1), 3604 (2019).