Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
Selpercatinib (LOXO-292; ARRY-192; Retevmo) is a potent,orally bioavailable and highly selective RET (REarranged during Transfection) tyrosin kinase inhibitor with IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib was given FDA approval in May 2020 to treat thyroid and lung cancers. The RET mutants and RET-containing fusion products that LOXO-292 specifically binds to and targets inhibit the growth of tumor cells that display elevated RET activity.
Targets |
RETWT (IC50 = 14.0 nM); RETV804M (IC50 = 24.1 nM); RETG810R (IC50 = 530.7 nM)
|
---|---|
ln Vitro |
Selpercatinib (LOXO-292) is a orally bioavailable, potent and selective RET kinase inhibitor.
|
ln Vivo |
Selpercatinib (LOXO-292; 10 mg/kg; i.g.; for 0-2 h) demonstrates favorable pharmacokinetics following oral gavage in FVB/NRj mice[1].
|
Cell Assay |
LOXO292 (1 µM) was added to the cells two hours prior to ALKAL2 or GDNF stimulation.
|
Animal Protocol |
Female nu/nu BALB/c mice
3 mg/kg o.g. |
References |
Molecular Formula |
C29H31N7O3
|
---|---|
Molecular Weight |
525.6015
|
Exact Mass |
525.25
|
Elemental Analysis |
C, 66.27; H, 5.95; N, 18.65; O, 9.13
|
CAS # |
2152628-33-4
|
Related CAS # |
2152628-33-4;2306313-13-1 (HCl);2306313-14-2 (sulfate);2306313-16-4; 2306313-17-5 (mesylate); 2306313-19-7 (besylate); 2306313-23-3; 2306313-28-8 (fumarate); 2306313-27-7 (tartrate); 2306313-29-9 (citrate)
|
Appearance |
Solid powder
|
SMILES |
CC(C)(COC1=CN2C(=C(C=N2)C#N)C(=C1)C3=CN=C(C=C3)N4CC5CC(C4)N5CC6=CN=C(C=C6)OC)O
|
InChi Key |
XIIOFHFUYBLOLW-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C29H31N7O3/c1-29(2,37)18-39-24-9-25(28-21(10-30)13-33-36(28)17-24)20-5-6-26(31-12-20)34-15-22-8-23(16-34)35(22)14-19-4-7-27(38-3)32-11-19/h4-7,9,11-13,17,22-23,37H,8,14-16,18H2,1-3H3
|
Chemical Name |
6-(2-hydroxy-2-methylpropoxy)-4-[6-[6-[(6-methoxypyridin-3-yl)methyl]-3,6-diazabicyclo[3.1.1]heptan-3-yl]pyridin-3-yl]pyrazolo[1,5-a]pyridine-3-carbonitrile
|
Synonyms |
LOXO-292; ARRY 192; LOXO292; ARRY192; LOXO 292; ARRY-192; Selpercatinib; Retevmo
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: 25~62.5 mg/mL (118.9~47.6 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO+40%PEG300+5%Tween80+50%ddH2O: 4.1mg/ml |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9026 mL | 9.5129 mL | 19.0259 mL | |
5 mM | 0.3805 mL | 1.9026 mL | 3.8052 mL | |
10 mM | 0.1903 mL | 0.9513 mL | 1.9026 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04280081 | Active Recruiting |
Drug: Selpercatinib | Solid Tumor Medullary Thyroid Cancer |
Loxo Oncology, Inc. | March 16, 2020 | Phase 2 |
NCT05906836 | Recruiting | Drug: Rosuvastatin Drug: Selpercatinib |
Healthy | Eli Lilly and Company | July 27, 2023 | Phase 1 |
NCT05668962 | Recruiting | Drug: Selpercatinib Drug: rhTSH |
Thyroid Cancer Thyroid Carcinoma |
Massachusetts General Hospital | March 1, 2023 | Phase 2 |
NCT03157128 | Recruiting | Drug: LOXO-292 | Colon Cancer Any Solid Tumor |
Loxo Oncology, Inc. | May 2, 2017 | Phase 1 Phase 2 |
NCT03899792 | Recruiting | Drug: LOXO-292 | Soft Tissue Sarcoma Infantile Fibrosarcoma |
Loxo Oncology, Inc. | June 13, 2019 | Phase 1 Phase 2 |