Selitrectinib (BAY 2731954; LOXO-195)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1650 | To Be Confirmed |
| 500mg | $2550 | To Be Confirmed |
| 1g | $3825 | To Be Confirmed |
: Cat #: V2684 CAS #: 2097002-61-2 Purity ≥ 98%
Description: Selitrectinib (also known as BAY-2731954; LOXO-195) is a 2nd generation, potent and selective TRK TKI (tyrosine kinase inhibitor) designed to overcome acquired resistance mediated by recurrent kinase domain (solvent front and xDFG) mutations identified in multiple patients who have developed resistance to other TRK TKIs such as larotrectinib (LOXO-101).
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- Related Biological Data
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| Molecular Weight (MW) | 380.43 |
|---|---|
| Molecular Formula | C20H21FN6O |
| CAS No. | 2097002-61-2 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: >60 mg/mLr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | FC1=CN=C(CC[C@@H](C)NC(C2=C3N(C=CC4=N3)N=C2)=O)C([C@@H]5N4CCC5)=C1 |
| Synonyms | LOXO-195; BAY-2731954; LOXO 195; BAY2731954; LOXO195; Selitrectinib; BAY 2731954 |
| Protocol | In Vitro | Selitrectinib (LOXO-195) demonstrates strong binding to the wild-type TRKA, TRKB and TRKC kinase domains. Selitrectinib (LOXO-195) has potent (IC50<1 nM) inhibitory activity in kinase enzyme assays. Importantly, Selitrectinib (LOXO-195) achieves low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, with IC50s ranging from 2.0-9.8 nM. 228 individual kinases in vitro are profiled at a Selitrectinib (LOXO-195) concentration of 1 μM, which is ~1667-fold higher than its IC50 for TRKA (0.6 nM). Selitrectinib (LOXO-195) is more than 1000-fold selective for 98% of non-TRK kinases tested. Selitrectinib (LOXO-195) demonstrates potent inhibition of cell proliferation in TRK fusion-containing KM12, CUTO-3, and MO-91 cell lines (IC50≤5 nM). |
|---|---|---|
| In Vivo | Stably transfected NIH-3T3 ΔTRKA and ΔTRKA-G595R cells are implanted subcutaneously into the flanks of nude mice. Both larotrectinib and Selitrectinib (LOXO-195) are effective at reducing phosphorylated TRKA in tumors driven by ΔTRKA. In contrast, only Selitrectinib (LOXO-195) strongly suppresses phospho-TRKA in ΔTRKA-G595R cells in a dose-dependent manner. Selitrectinib (LOXO-195) also causes inhibition of tumor growth relative to vehicle at all doses in four TRKA-dependent tumor models (ΔTRKA, ΔTRKA-G595R, ΔTRKAG667C, and TPM3-NTRK1 fusion-positive KM12 colorectal cancer cells. Larotrectinib inhibits KM12 and NIH 3T3-ΔTRKA tumors to a similar degree. Group mean body weight loss does not exceed 5% for any agent. Selitrectinib (LOXO-195) displays high selectivity for the TRK proteins. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.6286 mL | 13.1430 mL | 26.2860 mL | 52.5721 mL |
| 5mM | 0.5257 mL | 2.6286 mL | 5.2572 mL | 10.5144 mL |
| 10mM | 0.2629 mL | 1.3143 mL | 2.6286 mL | 5.2572 mL |
| 20mM | 0.1314 mL | 0.6572 mL | 1.3143 mL | 2.6286 mL |
The molarity calculator equation
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
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Average weight of animals g
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid 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 master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.