1. Protein Tyrosine Kinase/RTK
  2. Trk Receptor

LOXO-101 sulfate (Synonyms: Larotrectinib sulfate)

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

LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, 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 sulfate Chemical Structure

LOXO-101 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
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Estimated Time of Arrival: December 31
100 mg USD 840 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of LOXO-101 sulfate:

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  • References

Description

LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases. IC50 value: 2 - 20 nM Target: TRKA/B/C in vitro: LOXO-101 is an orally administered inhibitor of the TRK kinase and is highly selective only for the TRK family of receptors. LOXO-101 is 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. In the panel, LOXO-101 demonstrates greater than 50% inhibition for only one non-TRK kinase (TNK2 IC50, 576 nM). Measurement of proliferation following treatment with 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. [1] LOXO-101 demonstrates potent and highly-selective inhibition of TRKA, TRKB, and TRKC over other kinase- and non-kinase targets. 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. [2] in vivo: Athymic nude mice injected with KM12 cells are treated with LOXO-101 orally daily for 2 weeks. Dose-dependent tumor inhibition is observed, demonstrating the ability of this selective compound to inhibit tumor growth in vivo. [1]

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

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.
References
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:
LOXO-101 sulfate
Cat. No.:
HY-12866A
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LOXO-101 sulfate

Cat. No.: HY-12866A