MRTX0902
MRTX0902 Basic information
- Product Name:
- MRTX0902
- Synonyms:
-
- 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
- CAS:
- 2654743-22-1
- MF:
- C22H24N6O
- MW:
- 388.48
- Product Categories:
-
- APIS
- 1
- Mol File:
- 2654743-22-1.mol
More
Less
MRTX0902 Chemical Properties
- 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|
More
Less
MRTX0902 Usage And Synthesis
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]
| Parameter | Route | Dose (mg/kg) | Cl (mL/min/kg) | Vd,ss (L/kg) | T1/2(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 |
| 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
MRTX0902Supplier
Shanghai Tachizaki Biomedical Research Center Gold
- Tel
- 18014399201
- sales@chemlab-tachizaki.com
Chengdu DingDang Pharmaceutical Co., Ltd. Gold
- Tel
- 028-86040038 13980902949;
- market@dingdangchem.com
Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd Gold
- Tel
- 15317229551
- 15151849396@163.com
SuZhou GoodChemTech Co., Ltd Gold
- Tel
- 18136139868; 18136139868
- jinlun@goodchemtech.cn
Chengdu ruihede Medical Technology Co., Ltd Gold
- Tel
- 17381862311; 17381862311
- sales2@ruihede.cn