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HRS-4642


CAS No. : 2836263-09-1

2836263-09-1
Price and Availability of CAS No. : 2836263-09-1
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1mg $296 In-stock
5mg $420 In-stock
10mg $670 In-stock
25mg $1340 In-stock
50mg $2140 In-stock
100mg $3420 In-stock
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Cat. No. : HY-159127
M.Wt: 632.68
Formula: C34H35F3N6O3
Purity: >98 %
Solubility: DMSO : ≥ 100 mg/mL
Introduction of 2836263-09-1 :

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]. In Vitro:HRS-4642 selectively binds to *KRAS*G12D[2].
HRS-4642 inhibits KRASG12D binding to SOS1 or RAF1, blocking the downstream MEK-ERK signaling pathway[2].
HRS-4642 specifically inhibits the proliferation of *KRAS*G12D mutant human cell lines[2]. In Vivo:HRS-4642 (i.v.) exerts dose-dependent antitumor activity against KRASG12D-mutant AsPC-1 pancreatic cancer xenografts in nude mice with favorable tolerability[1].
HRS-4642 (2.5-15 mg/kg; i.v.; once a week) inhibits tumor growth in in BALB/c nude mice bearing KRAS G12D-mutant AsPC-1 (pancreatic cancer) and GP2d (colorectal cancer) tumors[3].

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