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Purity: ≥98%
MRTX0902 (MRTX-0902) is a novel, potent, selective, brain-penetrant, and orally bioavailable SOS1 binder that disrupts the SOS1:KRASG12C PPI (protein-protein interaction) with a binding Ki of 1.9 nM and IC50 of 29 nM in MKN1 cells. In the MIA PaCa-2 tumor mouse xenograft model, oral administration of MRTX0902 plus MRTX849 causes a notable increase in antitumor activity compared to that of either agent alone, including tumor regressions in a subset of animals. SOS1 is one of the major guanine nucleotide exchange factors that regulates the ability of KRAS to cycle through its 'on' and 'off' states. A compelling mechanistic reasoning exists for combining inhibitors of the SOS1:KRAS complex with inhibitors such as MRTX849 that target GDP-loaded KRASG12C, as disrupting the SOS1:KRASG12C protein–protein interaction (PPI) can increase the proportion of GDP-loaded KRASG12C.
| Targets |
KRAS-SOS1 ( IC50 = 46 nM )
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|---|---|
| ln Vitro |
MRTX0902 (compound 32) (1 μM; 0, 2, 4, 8, 15, and 30 minutes) exhibits a low lipophilicity with a cLogP of 3.4 and a moderate Clint value of 195 mL/min/kg in human liver microsomes[1].
MRTX0902 exhibits strong selectivity for SOS1 (Ki=2 nM) compared to SOS2 and EGFR (both Ki values >10,000 nM). MRTX0902 has an IC50 value of 29 nM, which is sufficient to inhibit MKN1 cells[1]. |
| ln Vivo |
MRTX0902 (compound 32) (25, 50 mg/kg; p.o. ; twice daily; 25 d), exhibits anti-tumor effect and causes tumor regression in mouse model[1].
MRTX0902 has good brain penetration, low clearance, and high bioavailability at 1-3 mg/kg for intravenous injection and 10-30 mg/kg for oral administration in a single dose[1]. |
| References |
| Molecular Formula |
C22H24N6O
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|---|---|
| Molecular Weight |
388.47
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| Exact Mass |
388.2
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| Elemental Analysis |
C, 68.02; H, 6.23; N, 21.63; O, 4.12
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| CAS # |
2654743-22-1
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| Related CAS # |
2654743-22-1
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C=CC=C1[C@@H](C)NC2=NN=C(C3=CN=C(C=C32)N4CCOCC4)C)C#N
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| InChi Key |
ILPWEAHQRAWJIU-OAHLLOKOSA-N
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| InChi Code |
InChI=1S/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-/m1/s1
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| Chemical Name |
2-methyl-3-[(1R)-1-[(4-methyl-7-morpholin-4-ylpyrido[3,4-d]pyridazin-1-yl)amino]ethyl]benzonitrile
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| Synonyms |
MRTX-0902; MRTX0902; MRTX 0902
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO 12.5~100 mg/mL (32.2~257.4 mM)
Ethanol: ~100 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5742 mL | 12.8710 mL | 25.7420 mL | |
| 5 mM | 0.5148 mL | 2.5742 mL | 5.1484 mL | |
| 10 mM | 0.2574 mL | 1.2871 mL | 2.5742 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05578092 | Completed | Drug: MRTX0902 Drug: MRTX849 |
Solid Tumor Colo-rectal Cancer Advanced Solid Tumor Non Small Cell Lung Cancer |
Mirati Therapeutics Inc. | November 4, 2022 | Phase 1 Phase 2 |
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