BiochemProbe — Life Science Research Reagents

MRTX0902 free base · Synonyms: MRTX-0902 · MRTX 0902

MRTX0902 is an effective SOS1 inhibitor.

For research use only. Not for human or veterinary use.

Target SOS1 Ras
Purity >98% Stock Inquire

MRTX0902 structure

CAS No.: 2654743-22-1

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
25 mg USD 450.00 BP-02360-25mg In stock Get quote
50 mg USD 650.00 BP-02360-50mg In stock Get quote
100 mg USD 900.00 BP-02360-100mg In stock Get quote
250 mg USD 1,350.00 BP-02360-250mg In stock Get quote
500 mg USD 2,150.00 BP-02360-500mg In stock Get quote
1 g Inquire BP-02360-1g In stock Inquire

Need another size or custom synthesis? Request a quote.

Description

MRTX0902 is an effective SOS1 inhibitor with an IC50 of 46 nM.

Biological activity

MRTX0902 is an oral brain penetrating SOS1:KRAS protein-protein interaction inhibitor with an IC50 of 46 nM. MRTX0902 displays high selectivity on SOS1 (Ki=2 nM) over SOS2 and EGFR (both Ki values >10,000 nM), MRTX0902 inhibits MKN1 cells with an IC50 value of 29 nM. MRTX0902 (25, 50 mg/kg; p.o.; twice daily; 25 d) shows anti-tumor effect in mouse model and results tumor regression.

Identifiers

SMILES
C[C@H](C1=C(C(C#N)=CC=C1)C)NC2=NN=C(C)C3=C2C=C(N4CCOCC4)N=C3
InChIKey
ILPWEAHQRAWJIU-OAHLLOKOSA-N

Specifications

MW (average)
388.4656
Formula
C22H24N6O
CAS No.
2654743-22-1
Physical state
Solid
Color
Light yellow to green yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro
DMSO 12.5 mg/mL

References

[1]. Ketcham JM, et al. Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction. J Med Chem. 2022 Jul 28;65(14):9678-9690.

Same target

Search SOS1

Same research area

Search Neurological Disease