Pan-RAS-IN-5
Pan-RAS-IN-5 is a macrocyclic pan-RAS inhibitor that targets mutant RAS (including KRAS, NRAS, and HRAS). Pan-RAS-IN-5 inhibits the proliferation of various KRAS-mutant cancer cells. Pan-RAS-IN-5 is applicable to the research of KRAS mutation-related cancers such as pancreatic cancer, nephroblastoma, and colon adenocarcinoma.
For research use only. We do not sell to patients.
- Formula: C45H58N8O5S
- Molecular Weight:823.06
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ASPC1 | IC50 |
6.6 nM
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Inhibited AsPC-1 cell proliferation.
Inhibited AsPC-1 cell proliferation.
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WO2024067857A1 |
| PSN1 | IC50 |
10.5 nM
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Inhibited PSN-1 cell proliferation.
Inhibited PSN-1 cell proliferation.
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WO2024067857A1 |
| LoVo | IC50 |
5.9 nM
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Inhibited LOVO cell proliferation.
Inhibited LOVO cell proliferation.
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WO2024067857A1 |
In Vitro
Pan-RAS-IN-5 (compound 7A) (10 μM to 0.128 nM, 5-fold serial dilution; 5 days) inhibits the proliferation of various KRAS-mutant cancer cells, with IC50 values of 6.6 nM, 10.5 nM, 7.5 nM and 5.9 nM against AsPC-1, PSN-1, RKN and LOVO cells, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Vd | CL | AUC0-last | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 8.5 h | 2.5 L/kg | 3.6 mL/min/kg | 4950 nM·h | / | / | / |
| Rat[1] | 10 mg/kg | p.o. | 7.3 h | / | / | 17069 nM·h | 1455 nM | 4.0 h | 34.2 % |
| Dog[1] | 1 mg/kg | i.v. | 10.3 h | 3.0 L/kg | 4.2 mL/min/kg | 4712 nM·h | / | / | / |
| Dog[1] | 5 mg/kg | p.o. | 12.0 h | / | / | 7632 nM·h | 618 nM | 1.0 h | 33.2 % |
Chemical Information
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Molecular Weight 823.06
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Formula C45H58N8O5S
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SMILES
O=C([C@@H](NC([C@H]1C[C@@H]1C)=O)CC2=NC(C3=CC(C(CC(C)(COC4=O)C)=[C@@]([C@@]5=C([C@@H](OC)C)N=CC(N6CCN(C)CC6)=C5)N7CC)=C7C=C3)=CS2)N8N[C@H]4C9CC8C9
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pan-RAS-IN-5 Related Classifications
HY-162536 Related Classifications
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