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(S)-AMG-510
🥰Excellent
Catalog No. T22258Cas No. 2252403-56-6
(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.
(S)-AMG-510
🥰Excellent
Purity: 98.57%
Catalog No. T22258Cas No. 2252403-56-6
(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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $31 | In Stock | |
| 5 mg | $48 | In Stock | |
| 10 mg | $77 | In Stock | |
| 25 mg | $158 | In Stock | |
| 50 mg | $288 | In Stock | |
| 100 mg | $449 | In Stock | |
| 500 mg | $987 | In Stock |
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Questions
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Purity:98.57%
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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 | (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. |
| In vitro | METHODS: KRAS G12 mutant NSCLC cell lines (NCI-H358 [G12C], NCI-H23 [G12C], NCI-H2122 [G12C], A549 [G12S], NCI-H2009 [G12A], NCI-H441 [G12V], and SK-LU1 [G12D]) were treated with (S)-AMG-510 (0.001-100000nM, 72 hours), and cell viability was detected by CCk8. RESULTS All non-G12C cell lines were as expected. Among KRAS G12 C cells, H358 and H2122 were sensitive, but H23 cells were resistant to (S)-AMG-510. METHODS: Engineered Ba/F3 cells carrying KRAS G12C were treated with (S)-AMG-510 (0.001-100000nM, 72 hours), and cell viability was determined by CCK8. RESULTS Ba/F3 cells expressing KRAS G12C were sensitive to sotorasib with an IC50 value of 12.4nM. METHODS: Ba/F3 cells expressing KRAS G12C or G12D were treated with (S)-AMG-510 (10-100nM, 6 hours) or adagrasib and immunoblotted. RESULTS (S)-AMG-510 inhibited pERK and pS6 levels in Ba/F3 cells expressing KRAS G12C; it had no effect on KRAS G12D. [3] |
| In vivo | METHODS: (S)-AMG-510 (10 mg/kg, oral) or sotorasib (10 mg/kg) + encorafenib (20 mg/kg) were used to treat NOD/SCID mice bearing tumor xenografts. The body weight and tumor size of the mice were monitored every 2 days. RESULTS (S)-AMG-510 withdrawal and the combination of BRAF inhibitors induced tumor regression in vivo. [4] |
| Molecular Weight | 560.59 |
| Formula | C30H30F2N6O3 |
| Cas No. | 2252403-56-6 |
| Smiles | O=C1N(C=2C(C(=N1)N3[C@@H](C)CN(C(C=C)=O)CC3)=CC(F)=C(N2)C4=C(F)C=CC=C4O)C5=C(C(C)C)N=CC=C5C |
| Relative Density. | 1.36 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 5.61 mg/mL (10 mM)  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(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.
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