ChemicalBook > CAS DataBase List > MRTX0902

MRTX0902

Product Name
MRTX0902
CAS No.
2654743-22-1
Chemical Name
MRTX0902
Synonyms
MRTX0902;MRTX0902 ，E1183;(R)-2-Methyl-3-[1-[(4-methyl-7-morpholinopyrido[3,4-d]pyridazin-1-yl)amino]ethyl]benzonitrile;(R)-2-Methyl-3-(1-((4-methyl-7-morpholin-4-ylpyrido[3,4-d]pyridazin-1-yl)amino)ethyl)-benzonitrile;Benzonitrile, 2-methyl-3-[(1R)-1-[[4-methyl-7-(4-morpholinyl)pyrido[3,4-d]pyridazin-1-yl]amino]ethyl]-
CBNumber
CB910828952
Molecular Formula
C22H24N6O
Formula Weight
388.48
MOL File
2654743-22-1.mol
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MRTX0902 Property

Boiling point:
658.0±55.0 °C(Predicted)
Density 
1.28±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:125.0(Max Conc. mg/mL);321.77(Max Conc. mM)
pka
7.93±0.30(Predicted)
form 
Solid
color 
Light yellow to green yellow
InChI
InChI=1/C22H24N6O/c1-14-17(12-23)5-4-6-18(14)15(2)25-22-19-11-21(28-7-9-29-10-8-28)24-13-20(19)16(3)26-27-22/h4-6,11,13,15H,7-10H2,1-3H3,(H,25,27)/t15-/s3
InChIKey
ILPWEAHQRAWJIU-UJHUVDBMNA-N
SMILES
N(C1=NN=C(C)C2C=NC(N3CCOCC3)=CC1=2)[C@@H](C1C=CC=C(C#N)C=1C)C |&1:18,r|
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

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MRTX0902 Chemical Properties,Usage,Production

Uses

MRTX0902 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10)[1].

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[1].
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[1].
PK Parameters for MRTX0902 across Species[1]

ParameterRouteDose (mg/kg)Cl (mL/min/kg)Vd,ss (L/kg)T1/2(iv) (h)F (%)
MouseIV/PO3/304.40.281.369
RatIV/PO1/1014.60.280.6283
DogIV/PO2/107.60.480.8638
Animal Model:Female CD-1 mice[1]
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 (T1/2= 1.3 h).
Animal Model:MIA PaCa-2 xenograft model in mouse[1]
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.

IC 50

KRAS-SOS1: 46 nM (IC50)

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. DOI:10.1021/acs.jmedchem.2c00741

MRTX0902 Preparation Products And Raw materials

Raw materials

Preparation Products

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MRTX0902 Suppliers

CHINA 75 United States 3 Global 78
Shanghai Tachizaki Biomedical Research Center
Tel
18014399201
Email
sales@chemlab-tachizaki.com
Country
China
ProdList
2769
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58
Chengdu DingDang Pharmaceutical Co., Ltd.
Tel
028-86040038 13980902949;
Fax
028-85149890
Email
market@dingdangchem.com
Country
China
ProdList
1854
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55
Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd
Tel
15317229551
Fax
QQ:3607245178
Email
15151849396@163.com
Country
China
ProdList
997
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58
SuZhou GoodChemTech Co., Ltd
Tel
18136139868; 18136139868
Email
jinlun@goodchemtech.cn
Country
China
ProdList
308
Advantage
58
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 18971495150;
Email
sales@sun-shinechem.com
Country
China
ProdList
1150
Advantage
64
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070 13770331960
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
16055
Advantage
64
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3505
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58
Bide Pharmatech Ltd.
Tel
400-400-164-7117 18317119277
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
ProdList
39999
Advantage
60
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4827
Advantage
55
Shanghaizehan biopharma technology co., Ltd.
Tel
021-61350663 13052117465
Fax
021-61350662
Email
sales@zehanbiopharma.com
Country
China
ProdList
977
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55
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View Lastest Price from MRTX0902 manufacturers

Hubei Chuchang Biotech Co., Ltd.
Product
MRTX0902 2654743-22-1
Price
US $0.00-0.00/MG
Min. Order
1MG
Purity
98
Supply Ability
100G
Release date
2024-04-17

2654743-22-1, MRTX0902Related Search:

Adagrasib BAM15 (3aR,6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide TG4-155 PH 797804 NVP-TAE684 MRTX1133 MRTX-1719 INDEX NAME NOT YET ASSIGNED MRTX-EX185

  • MRTX0902
  • Benzonitrile, 2-methyl-3-[(1R)-1-[[4-methyl-7-(4-morpholinyl)pyrido[3,4-d]pyridazin-1-yl]amino]ethyl]-
  • (R)-2-Methyl-3-[1-[(4-methyl-7-morpholinopyrido[3,4-d]pyridazin-1-yl)amino]ethyl]benzonitrile
  • MRTX0902 ，E1183
  • (R)-2-Methyl-3-(1-((4-methyl-7-morpholin-4-ylpyrido[3,4-d]pyridazin-1-yl)amino)ethyl)-benzonitrile
  • 2654743-22-1
  • APIS
  • 1