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RMC-9805 is a novel, mutant-selective, covalent and oral KRASG12D (ON) inhibitor. A stable and high affinity triple complex is formed between RMC-9805, KRASG12D, and cyclophilin A, which inhibits signal transduction downstream of KRASG12D (ON) by disrupting its interaction with downstream effectors. RMC-9805 can induce cell apoptosis and promote tumor regression in preclinical KRASG12D tumor models. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $132 | In Stock | |
5 mg | $328 | In Stock | |
10 mg | $562 | In Stock | |
25 mg | $1,280 | In Stock |
Description | RMC-9805 is a novel, mutant-selective, covalent and oral KRASG12D (ON) inhibitor. A stable and high affinity triple complex is formed between RMC-9805, KRASG12D, and cyclophilin A, which inhibits signal transduction downstream of KRASG12D (ON) by disrupting its interaction with downstream effectors. RMC-9805 can induce cell apoptosis and promote tumor regression in preclinical KRASG12D tumor models. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs. |
In vitro | METHODS: eCT26 (KRASG12D/G12D) and KPCY 6499c4 (KRASG12D/+) cells were treated with RMC-9805 (100 nM) for 48 hours, and cytokine levels were measured using a cytokine array. Cell surface expression was detected by flow cytometry.
RESULTS: CXCL1 and GM-CSF were reduced in eCT26 (KRASG12D/G12D) and KPCY 6499c4 (KRASG12D/+) cells, while PD-L1 and PVR were reduced; CXCL10 and CCL17 increased, while MHC-I and MHC-II increased. [2] |
In vivo | METHODS: To detect in vivo anti-tumor activity, RMC-9805 (100 mg/kg) was orally administered to eCT26 (KRASG12D/G12D) xenograft tumor mice once a day for 4-8 days.
RESULTS: RMC-9805 exhibits anti-tumor activity in the KRAS G12D xenograft model. [2] |
Alias | Zoldonrasib, KRAS G12D inhibitor 18, KRAS G12D IN 18 |
Molecular Weight | 1168.44 |
Formula | C63H88F3N11O7 |
Cas No. | 2922732-54-3 |
Smiles | C(C(F)(F)F)N1C(=C2C=3C1=CC=C(C3)N4C[C@](C[C@H](NC([C@@H](N5C[C@@]6(CC5)CN(C(=O)[C@H]7[C@H](N7C)[C@@H]8CC8)CC6)[C@H]9CCCC9)=O)C(=O)N%10N[C@](C(=O)OCC(C)(C)C2)(CCC%10)[H])(OCC4)[H])C%11=C([C@@H](OC)C)N=CC(=C%11)N%12CCN(CC%12)C%13CC%13 |
Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (85.58 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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