Larotrectinib sulfate (Synonyms: LOXO-101 (sulfate))

Cat. No.: HY-12866A Purity: 99.21%
Handling Instructions

Larotrectinib sulfate is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).

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

Larotrectinib sulfate Chemical Structure

Larotrectinib sulfate Chemical Structure

CAS No. : 1223405-08-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 97 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
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10 mg USD 144 In-stock
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50 mg USD 504 In-stock
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100 mg USD 840 In-stock
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Other Forms of Larotrectinib sulfate:

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Description

Larotrectinib sulfate is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).

In Vitro

Larotrectinib sulfate is an ATP-competitive oral inhibitor of the tropomyosin-related kinase (TRK) family of receptor kinases (TRKA, B, and C), with low nanomolar 50% inhibitory concentrations against all three isoforms, and 1,000-fold or greater selectivity relative to other kinases[1][2]. Measurement of proliferation following treatment with Larotrectinib sulfate demonstrates a dose-dependent inhibition of cell proliferation in all three cell lines. The IC50 is less than 100 nM for CUTO-3.29 and less than 10 nM for KM12 and MO-91 consistent with the known potency of this drug for the TRK kinase family[3].

In Vivo

In rat and monkey studies, Larotrectinib sulfate demonstrates 33-100% oral bioavailability and 60-65% plasma protein binding. It has low brain penetration, and is well tolerated in 28 day (d) GLP toxicology studies. A single dose (30 mg/kg) of Larotrectinib sulfate reduces tyrosine phosphorylation of TRKA and downstream signal transduction (pERK) in the tumor >80%[1]. Athymic nude mice injected with KM12 cells are treated with Larotrectinib sulfate orally daily for 2 weeks. Dose-dependent tumor inhibition is observed demonstrating the ability of this selective compound to inhibit tumor growth in vivo[4]. Larotrectinib sulfate (200mg/kg/day p.o for six weeks) reduces leukemic infiltration to undetectable levels in the bone marrow and spleen compared to vehicle-treated mice. Mice treated with Larotrectinib sulfate are still alive and leukemia-free four weeks after the cessation of treatment, as determined by Xenogen imaging[5].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (94.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8993 mL 9.4965 mL 18.9930 mL
5 mM 0.3799 mL 1.8993 mL 3.7986 mL
10 mM 0.1899 mL 0.9496 mL 1.8993 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3.25 mg/mL (6.17 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3.25 mg/mL (6.17 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.25 mg/mL (6.17 mM); Clear solution

Animal Administration
[4]

Mice[4]
Athymic nude mice are used throughout the study. 5×105 KM12 cells are injected subcutaneously into the dorsal flank area of the mice. Tumor volume is monitored by direct measurement with calipers and calculated by the formula: length × (width2)/2. Following the establishment of tumor and when the tumor size is between 150-200 mm2, mice are randomly selected to receive diluent, 60 mg/kg/dose or 200 mg/kg/dose of Larotrectinib sulfate. Larotrectinib sulfate is administered by oral gavage once daily for 14 days. After the last dose, tissue and blood are collected at 3, 6 and 24 hours post-treatment[4].

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

Molecular Weight

526.51

Formula

C₂₁H₂₄F₂N₆O₆S

CAS No.

1223405-08-0

SMILES

O=S(O)(O)=O.O=C(N1CC[[email protected]](O)C1)NC2=C3N=C(N4[[email protected]@H](C5=CC(F)=CC=C5F)CCC4)C=CN3N=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.21%

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Product Name:
Larotrectinib sulfate
Cat. No.:
HY-12866A
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Larotrectinib sulfate

Cat. No.: HY-12866A