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MRTX0902 - 99%, high purity , CAS No.2654743-22-1

COA

Grade & Purity:

Moligand™

≥99%

Cas Number: 2654743-22-1
Molecular Weight: 388.47
PubChem CID: 156526655

In stock

Item Number

M647526

Grouped product items
SKU	Size	Availability	Price
M647526-1mg	1mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$82.90
M647526-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$199.90
M647526-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$296.90
M647526-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$629.90
M647526-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$999.90
M647526-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,643.90

View related series

G Protein Related (287) GPCR/G Protein (3172) KRAS (55) Ras (143) SOS1 inhibitor (3)

Basic Description

Synonyms	UNII-CRG69FR93G \| (R)-2-Methyl-3-(1-((4-methyl-7-morpholinopyrido[3,4-d]pyridazin-1-yl)amino)ethyl)benzonitrile
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	MRTX0902 is an active and potent SOS1 inhibitor with an IC50 of 46 nM.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Product Description	MRTX0902 is an orally active and potent SOS1 inhibitor with an IC 50 of 46 nM (WO2021127429A1; Example 12-10) In Vitro MRTX0902 (compound 32) (1 μM; 0, 2, 4, 8, 15, and 30 minutes) shows a moderate Cl int value of 195 mL/min/kg in human liver microsome and a low lipophilicity with cLogP of 3.4. MRTX0902 displays high selectivity on SOS1 (K i =2 nM) over SOS2 and EGFR (both K i values >10,000 nM), MRTX0902 inhibits MKN1 cells with an IC 50 value of 29 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo MRTX0902 (compound 32) (25, 50 mg/kg; p.o.; twice daily; 25 d) shows anti-tumor effect in mouse model and results tumor regression . MRTX0902 (1-3 mg/kg for i.v. or 10-30 mg/kg for p.o.; single dose) exhibits good brain penetrance, low clearance, and high bioavailability . PK Parameters for MRTX0902 across Species Parameter Route Dose (mg/kg) Cl (mL/min/kg) V d,ss (L/kg) T 1/2 (iv) (h) F (%) Mouse IV/PO 3/30 4.4 0.28 1.3 69 Rat IV/PO 1/10 14.6 0.28 0.62 83 Dog IV/PO 2/10 7.6 0.48 0.86 38 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD-1 mice Dosage: 50 mg/kg Administration: Oral gavage; twice daily; 1 day Result: Resulted free drug exposure in the brain as well as the efflux ratio in the Caco-2 assay (ER = 1.5). Showed short half-life of the compound in mice (T 1/2 = 1.3 h). Animal Model: MIA PaCa-2 xenograft model in mouse Dosage: 25 mg/kg; 50 mg/kg Administration: Oral gavage; twice daily; 25 days Result: Reduced tumor growth by 41% and 53% at 25 mg/kg and 50 mg/kg administration. Form:Solid IC50& Target:KRAS-SOS1 46 nM (IC 50 )

Associated Targets(Human)

EGFR Tclin Epidermal growth factor receptor erbB1 (33727 Activities)

Discover Target: EGFR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MIA PaCa-2 (5949 Activities)

Explore this target

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mechanisms of Action

Mechanism of Action	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	References

Names and Identifiers

Smiles	CC1=C(C=CC=C1[C@@H](C)NC2=NN=C(C3=CN=C(C=C32)N4CCOCC4)C)C#N
Isomeric SMILES	CC1=C(C=CC=C1[C@@H](C)NC2=NN=C(C3=CN=C(C=C32)N4CCOCC4)C)C#N
PubChem CID	156526655
Molecular Weight	388.47

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	DMSO : 12.5 mg/mL (32.18 mM; ultrasonic and warming and heat to 60°C)
Molecular Weight	388.500 g/mol
XLogP3	2.800
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	4
Exact Mass	388.201 Da
Monoisotopic Mass	388.201 Da
Topological Polar Surface Area	87.000 Å²
Heavy Atom Count	29
Formal Charge	0
Complexity	587.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	1
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	1

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