Ret-IN-1 | CAS 2222755-14-6

Ret-IN-1

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Cat #: V3949 CAS #: 2222755-14-6 Purity ≥ 98%

Description: Ret-IN-1, a Selpercatinib analog, is a novel, potent, orally bioavailable and selective a RET kinase inhibitor with anticancer activity. It was mistakenly listed as LOXO-292 (ARRY-192 or Selpercatinib). It is an investigational drug in clinical development for the treatment of patients with cancers that harbor abnormalities in the rearranged during transfection (RET) kinase. 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. As of May 2020, Selpercatinib was approved by the US FDA for the treatment of lung and thyroid cancers. LOXO-292 selectively binds to and targets various RET mutants and RET-containing fusion products, which leads to an inhibition of cell growth of tumors cells that exhibit increased RET activity.

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Physicochemical and Storage Information
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Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	553.63
Molecular Formula	C29H31N9O3
CAS No.	2222755-14-6
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: > 10mM
	Water: N/A
	Ethanol: N/A
SMILES Code	N#CC1=C2C(C3=NC=C(N4CC(C5)N(CC6=CC=C(OC)N=C6)C5C4)N=C3)=CC(OC[C@H]7CNCCO7)=CN2N=C1
Synonyms	RET-IN-1

Related Biological Data

Pre-clinical characterization of RET inhibitor selectivity and antitumor activity.

Clinical activity of LOXO-292 in medullary thyroid cancer after acquired resistance to multikinase inhibitors.

Clinical activity of LOXO-292 in KIF5B-RET fusion-positive lung cancer metastatic to the brain.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.8063 mL	9.0313 mL	18.0626 mL	36.1252 mL
5mM	0.3613 mL	1.8063 mL	3.6125 mL	7.2250 mL
10mM	0.1806 mL	0.9031 mL	1.8063 mL	3.6125 mL
20mM	0.0903 mL	0.4516 mL	0.9031 mL	1.8063 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

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.