SOS1-IN-14 - 10mM in DMSO , CAS No.2793405-20-4

CAS: 2793405-20-4 Cat. No.: S656157 Formula: C₂₉H₂₉F₃N₆O₂ Peso molecolare: 550.57

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC 50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406

In Vitro

SOS1-IN-14 (compound 13c) exhibits cellular SOS1 inhibition with an IC 50 of 21 nM. SOS1-IN-14 has certain inhibition for CYP2D6, CYP2C9, CYP2C8 and CYP3A4 with IC 50 s of 2.5 μM, 6.5 μM, 43.3 μM and 54.3 μM, respectively, indicating that it has a certain risk of drug-drug interaction. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SOS1-IN-14 (50 mg/kg; p.o.; qd) exhibits 83.0% tumor suppression in Mia-paca-2 pancreas xenograft mice tumor models . SOS1-IN-14 shows a favorable pharmacokinetic profile with a bioavailability of 86.8% in beagles . Pharmacokinetic Parameters of SOS1-IN-14 (compound 13c) in ICR mice, Sprague-Dawley rats and Beagle dogs . ICR Mice Sprague–Dawley Rats Beagle Dogs Administration p.o., 50 mg/kg i.v., 2 mg/kg p.o., 10 mg/kg i.v., 2 mg/kg p.o., 20 mg/kg T max (h) 0.5 0.08 3 0.08 2 T 1/2 (h) 4.61 1.17 2.32 3.83 6.68 C max (μg/mL) 2670 1261 265 568 1840 AUC 0-24 (ng/mL·h) 32300 970 1683 2962 25725 CL (mL/min/kg) / 2068 / 11.3 / V ss (L/kg) / 2126 / 3.88 / F (%) / / 34.5 / 86.8 K el (h -1 ) 0.265 / / / / MRT (h) 4.67 / / / / MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c nude mice (KRAS G12C variant Mia-paca-2 xenograft models) Dosage: 50 mg/kg Administration: p.o.; q.d., for 21 days Result: Exhibited 83.0% tumor suppression. Showed better potent tumor suppression than BI-3406 .

IC50& Target:IC 50 : 3.9 nM (SOS1)

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC 50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

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

Nomi e identificatori

• Peso molecolare: 550.57

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

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

The CAS Number is 2793405-20-4, the molecular formula is C29H29F3N6O2, and the molecular weight is 550.57 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.