| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
MRTX9768 (0-250 nM) Results LU99 SDMA maintained clearance for 4 days after 3 hours of drug treatment (exhibiting cleft binding and prolonged PRMT5·MTA occupancy). MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; proliferation IC50 11 nM) with significant cycling in HCT116 MTAP-WT cells (SDMA IC50 544 nM; IC50 861 nM) [1].
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|---|---|
| ln Vivo |
In xenograft experiments, ischemia models with MRTX9768 exhibited fold suppression of SDMA in MTAP-del tumors, with variable SDMA regulation found in the bone marrow [1]. MRTX9768 (model dosages of 30 mg/kg in CD-1 mice and beagle dogs and 10 mg/kg in cynomolgus monkeys) had a favorable ADME profile. Tumors (such as astroblastoma)[1][2]. (>50% bioavailability in mice and dogs, moderate to high clearance, no change in RBC parameters up to effective concentration (1000 mg/kg)) [3]. MRTX9768 (100 mg/kg). , barrier, BID, 6/21 days) results in SDMA inhibition maintained for 3 days after termination [3].
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| References |
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| Molecular Formula |
C24H17FN6O
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|---|---|
| Molecular Weight |
424.429787397385
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| Exact Mass |
424.144
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| CAS # |
2629314-68-5
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| Related CAS # |
MRTX9768 hydrochloride
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| PubChem CID |
156151804
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| Appearance |
White to light brown solid powder
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| LogP |
2.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
32
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| Complexity |
810
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC2C=CC=CC=2C(C#N)=C1C1=C(C=NN1C)C1C=CC2C(NN=C(CN)C=2C=1)=O
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| InChi Key |
BPTYWAYMKBEXES-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H17FN6O/c1-31-23(22-18(10-26)15-5-3-2-4-13(15)9-20(22)25)19(12-28-31)14-6-7-16-17(8-14)21(11-27)29-30-24(16)32/h2-9,12H,11,27H2,1H3,(H,30,32)
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| Chemical Name |
2-[4-[4-(aminomethyl)-1-oxo-2H-phthalazin-6-yl]-2-methylpyrazol-3-yl]-3-fluoronaphthalene-1-carbonitrile
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~50 mg/mL (~117.81 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.89 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.89 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3561 mL | 11.7805 mL | 23.5610 mL | |
| 5 mM | 0.4712 mL | 2.3561 mL | 4.7122 mL | |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3561 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.
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