1. Protein Tyrosine Kinase/RTK
  2. Trk Receptor

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

Cat. No.: HY-12866 Purity: 98.92%
Handling Instructions

LOXO-101 is a potent, ATP competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.

For research use only. We do not sell to patients.
LOXO-101 Chemical Structure

LOXO-101 Chemical Structure

CAS No. : 1223403-58-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
5 mg USD 84 In-stock
10 mg USD 144 In-stock
50 mg USD 504 In-stock
100 mg USD 840 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of LOXO-101:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

LOXO-101 is a potent, ATP competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases. In vivo: A single dose (30 mg/kg) of LOXO-101 reduced tyrosine phosphorylation of TRKA and downstream signal transduction (pERK) in the tumor >80%. LOXO-101 was well tolerated up to 200 mg/kg/day for 14 d in this model. In vitro: LOXO-101 was evaluated for off-target kinase enzyme inhibition against a panel of 226 non-TRK kinases at a compound concentration of 1,000 nM and ATP concentrations near the Km for each enzyme. LOXO-101 demonstrated greater than 50% inhibition for only one non-TRK kinase (TNK2 IC50 = 576 nM).

Clinical Trial
References
Molecular Weight

428.44

Formula

C₂₁H₂₂F₂N₆O₂

CAS No.

1223403-58-4

SMILES

O=C(N1C[[email protected]@H](O)CC1)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

Solvent & Solubility

DMSO: ≥ 4.6 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.92%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LOXO-101
Cat. No.:
HY-12866
Quantity: