Shopping Cart
- Remove All
Your shopping cart is currently empty
MRTX-1257
Catalog No. T16143Cas No. 2206736-04-9
MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK/PD experiment.
MRTX-1257
Catalog No. T16143Cas No. 2206736-04-9
MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK/PD experiment.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $58 | In Stock | |
| 2 mg | $82 | In Stock | |
| 5 mg | $133 | In Stock | |
| 10 mg | $231 | In Stock | |
| 25 mg | $391 | In Stock | |
| 50 mg | $586 | In Stock | |
| 100 mg | $838 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $179 | In Stock |
Bulk & Custom
Add to Cart
Questions
View MoreInhibitors Related to "MRTX-1257"
T93032621928-55-8In house
MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.
- $197
Size
QTY
Sotorasib
Cited
AMG-510
T86842296729-00-3
Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.
- $31
Size
QTY
CitedKetoconazole Cited
Xolegel, R-41400, Extina, (±)-Ketoconazol
T067965277-42-1
Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.
- $33
Size
QTY
CitedCASIN
Pirl1-related Compound 2
T3971425399-05-9
CASIN (Pirl1-related Compound 2) is a specific inhibitor of GTPase Cdc42 (IC50: 2 uM).
- $32
Size
QTY
Salirasib
S-Farnesylthiosalicylic acid, FTS, Farnesyl Thiosalicylic Acid
T6163162520-00-5
Salirasib (Farnesyl Thiosalicylic Acid)(Ki=2.6 μM), an effective competitive prenylated protein methyltransferase (PPMTase) inhibitor, inhibits Ras methylation with potential antineoplastic activity.
- $30
Size
QTY
RMC6236
T746982765081-21-6
RMC-6236 is a potent RAS(ON)MULTI inhibitor with broad-spectrum inhibitory activity against RAS-GTP and can be used in cancer research.
- $297
Size
QTY
(S)-(-)-Perillyl alcohol
T828218457-55-1
(S)-(−)-Perillyl alcohol (Perillyl alcohol), a monoterpene found in lavender, inhibits Ras farnesylation, upregulates the mannose-6-phosphate receptor, induces apoptosis, and exhibits anti-cancer activity.
- $31
Size
QTY
BI-2493
T720612937344-16-4In house
BI-2493 is a highly selective pan-KRAS inhibitor and structural analog of BI-2865.BI-2493 exhibits antitumor activity and inhibits tumor cell growth and can be used in the study of cancerous diseases.BI-2493 is a highly selective pan-KRAS inhibitor and structural analog of BI-2865.
- $630
Size
QTY
Adagrasib Cited
MRTX849
T83692326521-71-3
Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.
- $59
Size
QTY
CitedCCG-257081
MRTF/SRF-IN-1, CCG257081, CCG 257081
T307781922098-90-5In house
CCG-257081 (MRTF/SRF-IN-1) is an inhibitor of cardiac myosin-related transcription factor and serum response factor (MRTF/SRF) that acts by inhibiting the Rho/MRTF/SRF pathway.CCG-257081 has shown efficacy in preventing bleomycin-induced fibrosis in several mouse models. CCG-257081 can be used in cancer prevention and fibrosis research.
- $129
Size
QTY
(S)-AMG-510
T222582252403-56-6
(S)-AMG-510 is the S-type compound of AMG-510 (Sotorasib), which effectively and selectively inhibits KRASG12C through covalent interaction with mutant cysteine, thereby promoting clinical efficacy in KRASG12C tumors.
- $31
Size
QTY
Deltarasin
T64621440898-61-2In house
Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
- $38
Size
QTY
Select Batch
Purity:99.07%
Contact us for more batch information
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK/PD experiment. |
| In vivo | MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups. MRTX-1257 dosed of 100 mg/kg daily causes complete responses that are maintained >70 days after cessation of treatment. MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) displays rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice . |
| Molecular Weight | 565.71 |
| Formula | C33H39N7O2 |
| Cas No. | 2206736-04-9 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 35 mg/mL (61.87 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
| |||||||||||||||||||||||||||||||
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Keywords
Preview
Related Tags: buy MRTX-1257 | purchase MRTX-1257 | MRTX-1257 cost | order MRTX-1257 | MRTX-1257 chemical structure | MRTX-1257 in vivo | MRTX-1257 formula | MRTX-1257 molecular weight
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.