2. Neuronal Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. Trk Receptor Apoptosis
  4. Larotrectinib sulfate

Larotrectinib sulfate  (Synonyms: LOXO-101 sulfate; ARRY-470 sulfate)

Cat. No.: HY-12866A Purity: 98.96%
COA Handling Instructions

Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 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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10 mM * 1 mL in DMSO USD 76 In-stock
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10 mg USD 110 In-stock
50 mg USD 220 In-stock
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Based on 8 publication(s) in Google Scholar

Other Forms of Larotrectinib sulfate:

Larotrectinib sulfate Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 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).

IC50 & Target[1][2]

TrkA

 

TrkB

 

TrkC

 

In Vitro

Larotrectinib (LOXO-101) 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 (LOXO-101) 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].

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

Larotrectinib sulfate Related Antibodies
In Vivo

In rat and monkey studies, Larotrectinib (LOXO-101) 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 (LOXO-101) 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 (LOXO-101) (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].

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

526.51

Appearance

Solid

Formula

C21H24F2N6O6S
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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

H2O : 2 mg/mL (3.80 mM; ultrasonic and adjust pH to 2 with 1M HCl)

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:  PBS

    Solubility: 12.5 mg/mL (23.74 mM); Clear solution; Need ultrasonic

  • 2.

    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

  • 3.

    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

  • 4.

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

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

  • 5.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

  • 6.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.96%

COA (258 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
References
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 (LOXO-101). Larotrectinib (LOXO-101) 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.
References
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Larotrectinib sulfate Related Classifications

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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Keywords:

Larotrectinib1223405-08-0LOXO-101ARRY-470LOXO101LOXO 101ARRY470ARRY 470Trk ReceptorApoptosisTropomyosin related kinase receptor Inhibitorinhibitorinhibit

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