2. Protein Tyrosine Kinase/RTK
  3. RET
  4. Selpercatinib

Selpercatinib  (Synonyms: LOXO-292)

Cat. No.: HY-114370 Purity: 99.87%
COA Handling Instructions

Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity.

For research use only. We do not sell to patients.

Selpercatinib Chemical Structure

Selpercatinib Chemical Structure

CAS No. : 2152628-33-4

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Solution
10 mM * 1 mL in DMSO USD 69 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Solid
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10 mg USD 100 In-stock
25 mg USD 220 In-stock
50 mg USD 350 In-stock
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Based on 5 publication(s) in Google Scholar

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Description

Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity[1][2].

IC50 & Target

IC50: 14.0 nM (RETWT), 24.1 nM (RETV804M), and 530.7 nM (RETG810R)[2]
In Vivo

Selpercatinib (LOXO-292; 10 mg/kg; i.g.; for 0-2 h) has good pharmacokinetics after oral gavage in FVB/NRj mice[1].
Pharmacokinetic Parameters of Selpercatinib in FVB/NRj mice[1].

Administration i.g. (10 mg/kg)
Tmax (h) 1.8
Cmax (ng/mL) 7862
AUC (ng·h/mL) 26649
FVB/NRj mice, 10 mg/kg i.g.[1]

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

Animal Model: Male FVB/NRj mice[1]
Dosage: 10 mg/kg
Administration: Oral gavage; for 7.5 min, 15 min, 30 min, 1 h and 2 h (Pharmacokinetic Analysis)
Result: Had good pharmacokinetics after oral gavage in FVB/NRj mice.
Clinical Trial
Molecular Weight

525.60

Appearance

Solid

Formula

C29H31N7O3
CAS No.
SMILES

N#CC1=C2C(C3=CC=C(N4CC(C5)N(CC6=CC=C(OC)N=C6)C5C4)N=C3)=CC(OCC(C)(O)C)=CN2N=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (118.91 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

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

Purity: 99.87%

COA (253 KB) HNMR (195 KB) LCMS (111 KB)

Handling Instructions (2659 KB)
References
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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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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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Keywords:

Selpercatinib2152628-33-4LOXO-292LOXO292LOXO 292RETanticancerRET (WT)RET (V804M)RET (G810R)FVB/NRj miceInhibitorinhibitorinhibit

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