Size | Price | |
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100mg | ||
250mg | ||
500mg |
Targets |
KRas G12C
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ln Vitro |
In several KRAS mutant cancer cells (NCI-H2030, MIA PaCa-2, SW1573, NCI-H23, and NCI-H358 cells), LC-2 causes endogenous KRASG12C to degrade, with DC50s ranging from 0.25 to 0.76 μM. A genuine PROTAC mechanism drives the degradation of KRASG12C induced by LC-2. Treatment with 2.5 μM of LC-2 is applied to MIA PaCa-2, NCI-H23, and SW1573 cells for 6, 24, 48, and 72 hours. Maximum KRAS degradation happened in less than 24 hours and continued for up to 72 hours in all three cell lines[1].
In homozygous and heterozygous KRAS mutant cell lines, LC-2-induced (2.5 μM; 6-24 hours) KRAS G12C degradation modifies Erk signaling[1]. |
References |
Molecular Formula |
C34H37CLFN7O4
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Molecular Weight |
662.15
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Exact Mass |
661.2579585
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CAS # |
2561529-96-0
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Related CAS # |
2561529-96-0
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Appearance |
solid
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SMILES |
C=C(C(=O)N1CCN(C[C@@H]1CC#N)C2=NC(=NC3=C2CCN(C3)C4=CC=CC5=C4C(=CC=C5)Cl)OC[C@@H]6CCCN6CCC(=O)O)F
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InChi Key |
CWTHNCSWSDACRS-DQEYMECFSA-N
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InChi Code |
InChI=1S/C34H37ClFN7O4/c1-22(36)33(46)43-18-17-42(19-24(43)10-13-37)32-26-11-15-41(29-9-3-6-23-5-2-8-27(35)31(23)29)20-28(26)38-34(39-32)47-21-25-7-4-14-40(25)16-12-30(44)45/h2-3,5-6,8-9,24-25H,1,4,7,10-12,14-21H2,(H,44,45)/t24-,25-/m0/s1
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Chemical Name |
3-[(2S)-2-[[7-(8-chloronaphthalen-1-yl)-4-[(3S)-3-(cyanomethyl)-4-(2-fluoroprop-2-enoyl)piperazin-1-yl]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-2-yl]oxymethyl]pyrrolidin-1-yl]propanoic acid
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Synonyms |
MRTX849 acid
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
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: ~130 mg/mL (~196.3 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.5102 mL | 7.5512 mL | 15.1023 mL | |
5 mM | 0.3020 mL | 1.5102 mL | 3.0205 mL | |
10 mM | 0.1510 mL | 0.7551 mL | 1.5102 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 |
NCT04793958 | Recruiting | Biological: Cetuximab Drug: MRTX849 |
Advanced Colorectal Cancer Metastatic Colorectal Cancer |
Mirati Therapeutics Inc. | March 15, 2021 | Phase 3 |
MRTX849-VHL PROTACs engage and degrade endogenous KRASG12C in NCI-H2030 cells. td> |