Documents & Downloads

APS03118

RET Inhibitor

APS03118 is a potent and selective inhibitor of the rearranged during transfection (RET) oncogene, targeting various RET fusions and mutations, including G810, V804, L730, and Y806, with IC50 values primarily below 1 nM. This compound effectively inhibits the entire RET signaling cascade, including RET itself, Shc, and ERK1/2, while displaying over 20-fold selectivity against most off-target kinases. In preclinical studies, APS03118 demonstrated the ability to induce complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient-derived xenografts and significantly extend survival in models of intracranial CCDC6-RET metastasis. This reagent is suitable for research into RET-driven cancers, particularly in the context of selective RET inhibitor-resistant scenarios.

Out of Stock

Free Aliquoting for Your Order

Tell us your preferred amount per vial. We’ll confirm the options.

Specifications

Manufacturer	Adooq Bioscience
Actions	Inhibitor
CAS Number	2598870-24-5
Applications	RET Inhibitor
Formula	C₂₇H₂₈N₈O₂
Molecular Weight	496.56
SMILES	CCOC1=CN2NC3=NN=CC3=C2C(C4=CC=C(N5CC6N(C(C6)C5)CC7=CN=C(C=C7)OC)N=C4)=C1

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.