(S)-JDQ-443 , CAS No.2653994-10-4

CAS: 2653994-10-4 Cat. No.: J650946 Formula: C₂₉H₂₈ClN₇O Peso molecolare: 526.03

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Panoramica

(S)-JDQ-443 is an isomer of JDQ-443 . JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity.

In Vitro

JDQ-443 promotes dose-dependent reductions of phosphorylated ERK (pERK) levels and the proliferation of the KRASG12C-mutated cell lines NCI-H358 and NCI-H2122, with IC 50 values of 0.018 and 0.063 μM, respectively. JDQ443 covalently and selectively binds and inhibits GDP-bound KRASG12C with low reversible binding affinity to the RAS switch II pocket, and also inhibits proliferation of KRASG12C-mutated and KRAS G12C/H95, G12C/R68S, and G12C/Y96 double-mutant cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JDQ443 (10-100 mg/kg, Orally, daily for 14 days) shows antitumor activity and inhibits the growth of tumor in a dose-dependent manner in KRAS G12C-mutated CDX models. JDQ443 (Orally, 100 mg/kg, daily (JDQ443) + 7.5 mg/kg, twice daily (TNO155), for 36 days) shows greater cell growth inhibition or cell killing compared with single-agent JDQ443 when combined with TNO155. JDQ443 generates categorical antitumor responses in PDX models of NSCLC and colorectal tumors that are improved by combination treatment with other agents. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

Specifications

Meccanismi biochimici e fisiologici

(S)-JDQ-443 is an isomer of JDQ-443 ( HY-139612 ). JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity.

Condizioni di conservazione di stoccaggio

Store at -20°C

Spedito in

Ice chest + Ice pads

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

INHIBITOR

Nomi e identificatori

Peso molecolare

526.03

Domande frequenti

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2653994-10-4, the molecular formula is C29H28ClN7O, and the molecular weight is 526.03 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.