2836263-09-1
Chemical Structure
HRS-4642
- CAS No.: 2836263-09-1
- Formula:C34H35F3N6O3
- Molecular Weight:632.68
InChIKey: XLWBILUNGOIIFR-OWBPVYLJSA-N
SMILES: OC(C=C1C2=C(F)C(N=C(OC[C@@]3(CCC4)N4C[C@H](F)C3)N=C5N(C[C@@H]6N[C@H]7CC6)[C@@H]7CO8)=C5C8=N2)=CC9=C1C(CC)=C(F)C=C9
Biological Activity: HRS-4642 is a high affinity, selective, long-acting, and non-covalent KRASG12D inhibitor with a Kd value of 0.083 nM. HRS-4642 inhibits the binding of KRASG12D to SOS1 or RAF1, thereby blocking the downstream MEK-ERK signaling pathway. HRS-4642 promotes Apoptosis. HRS-4642 alone or combined with Carfilzomib (HY-10455) effectively shapes the tumor microenvironment. HRS-4642 has an anti-cancer effect on pancreatic and colorectal cancers carrying the KRASG12D mutation[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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HRS-4642 | 99.74% | HRS-4642 is a high affinity, selective, long-acting, and non-covalent KRASG12D inhibitor with a Kd value of 0.083 nM. HRS-4642 inhibits the binding of KRASG12D to SOS1 or RAF1, thereby blocking the downstream MEK-ERK signaling pathway. HRS-4642 promotes Apoptosis. HRS-4642 alone or combined with Carfilzomib (HY-10455) effectively shapes the tumor microenvironment. HRS-4642 has an anti-cancer effect on pancreatic and colorectal cancers carrying the KRASG12D mutation. | ||||||||||||||||||||
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- [1]. Zhou C, et al. Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. Cancer Cell. 2024 Jul 8;42(7):1286-1300.e8. [Content Brief]
- [2]. Leng Q, et al. HRS-4642 combined with nimotuzumab in the treatment of recurrent or metastatic pancreatic ductal adenocarcinoma: study protocol of a single-arm, prospective phase Ib/II trial. Front Pharmacol. 2025;16:1562481. Published 2025 Jul 4. [Content Brief]
- [3]. Li Y, et al. New exploration of KRASG12D inhibitors and the mechanisms of resistance. Exp Hematol Oncol. 2025;14(1):39. Published 2025 Mar 17. [Content Brief]
Keywords
