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KRas
KRas製品
- All (55)
- KRas阻害剤 (51)
- KRas作動薬(1)
- 新製品
| 製品コード | 製品名称 | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|---|
| S8830 | AMG 510 (Sotorasib) | Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. | ||
| S2797 | Lonafarnib (SCH66336) | Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3. |
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| S8707 | ARS-1620 | ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C) and could achieve rapid and sustained in vivo target occupancy to induce tumor regression. | ||
| S8884 | Adagrasib (MRTX849) | Adagrasib (MRTX849) is a potent, selective, and covalent KRAS G12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C and inhibits KRAS-dependent signaling. | ||
| S7224 | Deltarasin | Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. | ||
| S8156 | ARS-853 | ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis. | ||
| S8916 | BI-3406 | BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities. | ||
| E1051 | MRTX1133 | MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS. | ||
| S8826 | BAY-293 | BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM. | ||
| S7331 | K-Ras(G12C) inhibitor 12 | K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
-inhibitor-12-S733101W0420171213.gif)
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| S8499 | KRpep-2d | KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM. | ||
| S8955 | Sotorasib (AMG510) racemate | Sotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. | ||
| S8959 | BI-2852 | BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells. | ||
| S7332 | K-Ras(G12C) inhibitor 9 | K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C). | ||
| E1474 | BI-2865 | BI-2865 is a none-covalent pan-KRAS Inhibitor. It binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively and inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 ce | ||
| S6996 | LC-2 | LC-2 is a first PROTAC capable of degrading endogenous KRASG12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRASG12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRASG12C degradation leading to suppression of MAPK signaling. | ||
| S0023 | K-Ras-IN-1 | K-Ras-IN-1 (MDK-3017) inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. | ||
| E1187 | Divarasib (GDC-6036) | Divarasib (GDC-6036, RG6330) is a KRAS G12C inhibitor that binds irreversibly to switch II pocket of KRAS G12C (when in the inactive GDP-bound state) thereby blocking GTP binding and activation. | ||
| E1433 | LY3537982 (KRAS G12C Inhibitor 67) | LY3537982 (KRAS G12C inhibitor 19) is a highly selective and potent inhibitor of the KRAS-G12C protein. LY3537982 selectively inhibits the growth of KRAS G12C mutant cells H23 G12C, H358 G12C, and H2122 G12C with IC50s of 1.04 nM, 1.16 nM, and 11.38 nM, respectively. | ||
| E1578 | garsorasib (D-1553) | Garsorasib (D-1553 ) is a potent and selective oral KRASG12C inhibitor with antitumor activity. It has the potential to treat KRAS G12C-mutated non-small cell lung cancer (NSCLC). | ||
| E8295New | LY3499446 | LY3499446 (KRASG12C IN-13) is a potent inhibitor of KRAS G12C. It can be used in research on advanced solid tumors, including non-small cell lung cancer (NSCLC) and colorectal cancer (CRC). | ||
| E1606 | Elironrasib (RMC-6291) | RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). | ||
| S7330 | 6H05 | 6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C). | ||
| S7333 | K-Ras(G12C) inhibitor 6 | K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C). | ||
| E4758New | ACBI3 | ACBI3 is a selective and potent PROTAC degrader of pan-KRAS that promotes VHL engagement, ternary complex formation, and E3 ligase-dependent KRAS degradation with high proteome-wide selectivity. It demonstrates strong anti-tumor activity, resulting in durable pathway modulation and tumor regressions in KRAS driven cancers. | ||
| E1858 | RMC-7977 | RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RASMULTI (ON) inhibitor). It also exhibits significant anti-tumor efficacy in pancreatic ductal adenocarcinoma (PDAC). | ||
| E1857 | TH-Z816 | TH-Z816 is an inhibitor of ,KRAS(G12D) with an IC50 of 14 μM in an SOS-catalyzed nucleotide exchange assay with GDP as the incoming nucleotide. | ||
| E1356 | BI-0474 | BI-0474 is a potent inhibitor of KRASG12C with an IC50 value of 7.0 nM. It inhibits GDP-KRAS::SOS1 protein-protein interactions. It exhibits anti-proliferative and anti-tumour activity and can be used in cancer research. | ||
| E4651 | HRS-4642 | HRS-4642 is a selective inhibitor of KRAS G12D with a Kd value of 0.083 nM. It exhibits robust anti-cancer activity against KRAS G12D-mutant cancers both in vitro and in vivo. | ||
| E6405New | AZD0022 | AZD0022 is a potent, orally bioavailable, selective, reversible inhibitor of KRASG12D that drives robust pathway inhibition and anti-tumour activity in KRASG12D models. | ||
| E6406New | AMG 410 | AMG410 is a non-covalent, selective inhibitor of pan-KRAS with IC50 of 1–4 nM for KRAS G12D, G12V, and G13D. It binds both GDP- and GTP-bound KRAS with Kd of 1 nM and 22 nM, respectively. AMG410 inhibits KRAS signaling in a nucleotide cycling-independent manner. It also suppresses proliferation in KRAS-amplified wild-type tumor cells. | ||
| E1959New | RMC-4998 | RMC-4998 is a tri-complex inhibitor that selectively targets the GTP-bound state of mutant KRASG12C, with high potency for KRASG12C-CYPA tri-complex formation with an IC50 of 28 nM. It strongly inhibits ERK signaling with an IC50 of 1–10 nM and attenuates AKT/MTOR and RAL pathways, leading to potent suppression of KRASG12C-driven tumor growth and can used in cancer research. | ||
| E1056 | Opnurasib (JDQ-443) | Opnurasib (JDQ-443,NVP-JDQ443) , a potent and selective, orally bioavailable covalent inhibitor of GDP-bound KRASG12C with an IC50 of 0.012 µM for inhibition of c-Raf recruitment. | ||
| E1843New | Fulzerasib | Fulzerasib (IBI351, GFH925) is an irreversible small molecule inhibitor for KRAS G12C mutation blocking KRAS pathway signaling pERK with an IC50 of 37 nM. It demonstrates potent anti-tumor activity in multiple KRAS G12C-mutant tumor models including human pancreatic cancer, human lung adenocarcinoma, colorectal adenocarcinoma, and lung cancer models. | ||
| E1597 | Daraxonrasib (RMC-6236) | Daraxonrasib (RMC-6236) is a RAS(ON) multi-selective noncovalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS isoforms with broad therapeutic potential. RMC-6236 exhibits strong anticancer efficacy in RAS-addicted cell lines, especially those with mutations at codon 12 of KRAS. This product has successfully grown high-quality single crystals and solved their structures, revealing the three-dimensional spatial relationship of atoms in molecules and being able to directly and absolutely determine their chemical structure and stereo configuration. | ||
| E1576New | LUNA18 | LUNA18 (Paluratide) is an orally bioavailable 11-mer cyclic peptide KRAS inhibitor for the intracellular tough target RAS. It binds to KRASG12D with a kd of 0.043 nM and blocks KRASG12D–SOS1 interaction at IC50 of < 2.2 nM. It also exhibits antiproliferative activity in KRAS-mutant cancer cell lines with an IC50 of 1.4 nM in AsPC-1 pancreatic cancer cells. | ||
| S5279 | Fendiline hydrochloride | Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras. | ||
| E4697 | RGT-018 | RGT-018, is a potent and selective inhibitor of SOS1. It blocks the interaction of KRAS:SOS1 with an IC50 of 8 nM and inhibited KRAS signaling and the proliferation of KRAS-driven cancer cells. It may exhibit potent anticancer activity against NSCLC, colorectal cancer, and pancreatic cancer. | ||
| E1677 | Glecirasib | Glecirasib (JAB-21822, KRAS G12C inhibitor 36) is a potent, and highly selective, covalent inhibitor of KRAS G12C. It exhibits promising anti-tumor activity in KRAS G12C-mutated pancreatic ductal adenocarcinoma (PDAC) , Non-Small Cell Lung Cancer(NSCLC), Colorectal Cancer (CRC) and other solid tumors. | ||
| E1829New | Calderasib (MK-1084) | Calderasib (MK-1084) is a selective KRAS G12C inhibitor demonstrating antitumor efficacy. It can be utilized as monotherapy or in combination with pembrolizumab () for oncology research. | ||
| E2540New | Salvianolic acid F | サルビアノール酸FはKRAS阻害剤であり、特にKRAS G12Dに対して有効です。サルビアノール酸Fは同時にNF-κB、MMP-9、およびNOを阻害します。サルビアノール酸Fは、in vitroでEP300/PI3K/AKT経路を介して癌細胞の増殖、浸潤、および遊走を阻害し、アポトーシスを誘導します。サルビアノール酸Fは、in vivoでPI3K/AKTシグナル伝達経路を介してKRAS依存性肺癌細胞の増殖を阻害します。サルビアノール酸Fは、KRAS G12Dによって駆動される非小細胞肺癌（NSCLC）や卵巣癌を含む様々な癌の研究に使用できます。 | ||
| E1856 | ARS-1323 | ARS-1323 is the racemic mixture, containing ARS-1620, and a potent inhibitor of mutant KRAS G12C. It can be used in research for biochemical binding screens as companion imaging drugs (CID) for KRAS G12C. | ||
| E6643New | SS-3091 | SS - 3091はパンKRas阻害剤です。SS - 3091はKRasの相互作用界面に結合し、ARaf/KRas複合体を不安定化させ、それにより下流のシグナル伝達に影響を与えます。SS - 3091は、様々な癌細胞におけるKRas G12D、G12C、G12V、およびG12S変異体に対して有意な抗癌および抗増殖活性を有します。 | ||
| E1071 | ASP2453 | ASP2453, a potent, selective and covalent KRAS G12C inhibitor, inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf. ASP2453 is a potential therapeutic agent for KRAS G12C-mutated cancer. | ||
| E6526New | MCB-294 | MCB - 294は、NRASおよびHRASよりも選択的にKRASを阻害する二状態型パンKRAS阻害剤です。MCB - 294は、KRASの活性型（GTP結合型）と不活性型（GDP結合型）の両方に結合することができ、それぞれの解離定数（Kd）は約1 pMと10 nMです。MCB - 294は、G12D、G12C、G12V、G12S、G13Dおよび野生型KRASを発現するhTERT - HPNE細胞の増殖を広範囲に阻害し、IC50は約700 nMです。MCB - 294は、KRAS変異腫瘍において不可逆的なアポトーシスを誘導します。MCB - 294は、KRASG12C阻害剤耐性癌細胞を効果的に抑制し、腫瘍免疫微小環境を改変します。MCB - 294は、膵臓癌、結腸直腸癌および肺癌の研究に使用することができます。 | ||
| E6411New | RP03707 | RP03707は、PROTACベースのKRASG12D分解剤です（赤色：KRASG12D阻害剤 (HY - 134813)、黒色：リンカー、青色：E3リガーゼリガンド）。 | ||
| E5847New | olomorasib | Olomorasib (KRAS G12C inhibitor 19, LY3537982) is a potent and highly selective second-generation inhibitor of GDP-bound KRAS G12C, with the potential to treat patients with advanced solid tumors carrying the KRAS G12C mutation. | ||
| E6638New | VS-7375 (GFH375) | VS-7375 (GFH375) is an oral small-molecule inhibitor that selectively targets KRAS G12D in both its active (GTP-bound) and inactive (GDP-bound) forms. This dual-state inhibition results in stronger tumor suppression compared to single-state inhibitors. It exhibits potent anti-proliferative and anti-tumor effects in KRAS G12D-mutant models, including an intracranial GP2D tumor model. | ||
| E1968New | BBO-8520 | BBO-8520 is a covalent small molecule inhibitor that selectively targets KRAS G12C with high oral bioavailability. It functions as both a KRAS G12C (OFF) inhibitor and a blocker of KRAS G12C (ON) signaling. The compound inhibits cellular proliferation by binding to GTP-bound KRAS G12C (ON), thereby preventing RAS-RAF1 interaction and promoting the transition to the inactive (OFF) state . | ||
| E5910New | KRAS-533 | KRAS-533 is a potent agonist of KRAS that binds to the GTP/GDP-binding pocket and prevents the hydrolysis of GTP, leading to accumulation of active GTP-bound KRAS. This triggers both apoptotic and autophagic cell death pathways in cancer cells, leading to potent suppression of mutant KRAS lung cancer in vitro and in animal models. | ||
| E1157 | Pan-RAS-IN-1 | Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins. | ||
| E1962 | Zoldonrasib (RMC-9805) | Zoldonrasib (RMC-9805) is an orally active inhibitor of KRAS G12D. RMC-9805 inhibits RAS signaling, leading to apoptosis in cancer cells with the KRAS G12D mutation. | ||
| S8831 | MRTX-1257 | MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. | ||
| E1564 | BI-2493 | BI-2493, a structural analogue of BI-2865, is a highly selective inhibitor of pan-KRAS. BI-2493 attenuates tumor growth and can be used for cancer research. | ||
| E5910New | KRAS-533 | KRAS-533 is a potent agonist of KRAS that binds to the GTP/GDP-binding pocket and prevents the hydrolysis of GTP, leading to accumulation of active GTP-bound KRAS. This triggers both apoptotic and autophagic cell death pathways in cancer cells, leading to potent suppression of mutant KRAS lung cancer in vitro and in animal models. | ||
| S8830 | AMG 510 (Sotorasib) | Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. | ||
| S2797 | Lonafarnib (SCH66336) | Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3. |
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| S8707 | ARS-1620 | ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C) and could achieve rapid and sustained in vivo target occupancy to induce tumor regression. | ||
| S8884 | Adagrasib (MRTX849) | Adagrasib (MRTX849) is a potent, selective, and covalent KRAS G12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C and inhibits KRAS-dependent signaling. | ||
| S7224 | Deltarasin | Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ. | ||
| S8156 | ARS-853 | ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis. | ||
| S8916 | BI-3406 | BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities. | ||
| E1051 | MRTX1133 | MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS. | ||
| S8826 | BAY-293 | BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM. | ||
| S7331 | K-Ras(G12C) inhibitor 12 | K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
-inhibitor-12-S733101W0420171213.gif)
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| S8499 | KRpep-2d | KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM. | ||
| S8955 | Sotorasib (AMG510) racemate | Sotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. | ||
| S8959 | BI-2852 | BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells. | ||
| S7332 | K-Ras(G12C) inhibitor 9 | K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C). | ||
| E1474 | BI-2865 | BI-2865 is a none-covalent pan-KRAS Inhibitor. It binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively and inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 ce | ||
| S0023 | K-Ras-IN-1 | K-Ras-IN-1 (MDK-3017) inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. | ||
| E1187 | Divarasib (GDC-6036) | Divarasib (GDC-6036, RG6330) is a KRAS G12C inhibitor that binds irreversibly to switch II pocket of KRAS G12C (when in the inactive GDP-bound state) thereby blocking GTP binding and activation. | ||
| E1433 | LY3537982 (KRAS G12C Inhibitor 67) | LY3537982 (KRAS G12C inhibitor 19) is a highly selective and potent inhibitor of the KRAS-G12C protein. LY3537982 selectively inhibits the growth of KRAS G12C mutant cells H23 G12C, H358 G12C, and H2122 G12C with IC50s of 1.04 nM, 1.16 nM, and 11.38 nM, respectively. | ||
| E1578 | garsorasib (D-1553) | Garsorasib (D-1553 ) is a potent and selective oral KRASG12C inhibitor with antitumor activity. It has the potential to treat KRAS G12C-mutated non-small cell lung cancer (NSCLC). | ||
| E8295New | LY3499446 | LY3499446 (KRASG12C IN-13) is a potent inhibitor of KRAS G12C. It can be used in research on advanced solid tumors, including non-small cell lung cancer (NSCLC) and colorectal cancer (CRC). | ||
| E1606 | Elironrasib (RMC-6291) | RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). | ||
| S7330 | 6H05 | 6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C). | ||
| S7333 | K-Ras(G12C) inhibitor 6 | K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C). | ||
| E1858 | RMC-7977 | RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RASMULTI (ON) inhibitor). It also exhibits significant anti-tumor efficacy in pancreatic ductal adenocarcinoma (PDAC). | ||
| E1857 | TH-Z816 | TH-Z816 is an inhibitor of ,KRAS(G12D) with an IC50 of 14 μM in an SOS-catalyzed nucleotide exchange assay with GDP as the incoming nucleotide. | ||
| E1356 | BI-0474 | BI-0474 is a potent inhibitor of KRASG12C with an IC50 value of 7.0 nM. It inhibits GDP-KRAS::SOS1 protein-protein interactions. It exhibits anti-proliferative and anti-tumour activity and can be used in cancer research. | ||
| E4651 | HRS-4642 | HRS-4642 is a selective inhibitor of KRAS G12D with a Kd value of 0.083 nM. It exhibits robust anti-cancer activity against KRAS G12D-mutant cancers both in vitro and in vivo. | ||
| E6405New | AZD0022 | AZD0022 is a potent, orally bioavailable, selective, reversible inhibitor of KRASG12D that drives robust pathway inhibition and anti-tumour activity in KRASG12D models. | ||
| E6406New | AMG 410 | AMG410 is a non-covalent, selective inhibitor of pan-KRAS with IC50 of 1–4 nM for KRAS G12D, G12V, and G13D. It binds both GDP- and GTP-bound KRAS with Kd of 1 nM and 22 nM, respectively. AMG410 inhibits KRAS signaling in a nucleotide cycling-independent manner. It also suppresses proliferation in KRAS-amplified wild-type tumor cells. | ||
| E1959New | RMC-4998 | RMC-4998 is a tri-complex inhibitor that selectively targets the GTP-bound state of mutant KRASG12C, with high potency for KRASG12C-CYPA tri-complex formation with an IC50 of 28 nM. It strongly inhibits ERK signaling with an IC50 of 1–10 nM and attenuates AKT/MTOR and RAL pathways, leading to potent suppression of KRASG12C-driven tumor growth and can used in cancer research. | ||
| E1056 | Opnurasib (JDQ-443) | Opnurasib (JDQ-443,NVP-JDQ443) , a potent and selective, orally bioavailable covalent inhibitor of GDP-bound KRASG12C with an IC50 of 0.012 µM for inhibition of c-Raf recruitment. | ||
| E1843New | Fulzerasib | Fulzerasib (IBI351, GFH925) is an irreversible small molecule inhibitor for KRAS G12C mutation blocking KRAS pathway signaling pERK with an IC50 of 37 nM. It demonstrates potent anti-tumor activity in multiple KRAS G12C-mutant tumor models including human pancreatic cancer, human lung adenocarcinoma, colorectal adenocarcinoma, and lung cancer models. | ||
| E1597 | Daraxonrasib (RMC-6236) | Daraxonrasib (RMC-6236) is a RAS(ON) multi-selective noncovalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS isoforms with broad therapeutic potential. RMC-6236 exhibits strong anticancer efficacy in RAS-addicted cell lines, especially those with mutations at codon 12 of KRAS. This product has successfully grown high-quality single crystals and solved their structures, revealing the three-dimensional spatial relationship of atoms in molecules and being able to directly and absolutely determine their chemical structure and stereo configuration. | ||
| E1576New | LUNA18 | LUNA18 (Paluratide) is an orally bioavailable 11-mer cyclic peptide KRAS inhibitor for the intracellular tough target RAS. It binds to KRASG12D with a kd of 0.043 nM and blocks KRASG12D–SOS1 interaction at IC50 of < 2.2 nM. It also exhibits antiproliferative activity in KRAS-mutant cancer cell lines with an IC50 of 1.4 nM in AsPC-1 pancreatic cancer cells. | ||
| S5279 | Fendiline hydrochloride | Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras. | ||
| E4697 | RGT-018 | RGT-018, is a potent and selective inhibitor of SOS1. It blocks the interaction of KRAS:SOS1 with an IC50 of 8 nM and inhibited KRAS signaling and the proliferation of KRAS-driven cancer cells. It may exhibit potent anticancer activity against NSCLC, colorectal cancer, and pancreatic cancer. | ||
| E1677 | Glecirasib | Glecirasib (JAB-21822, KRAS G12C inhibitor 36) is a potent, and highly selective, covalent inhibitor of KRAS G12C. It exhibits promising anti-tumor activity in KRAS G12C-mutated pancreatic ductal adenocarcinoma (PDAC) , Non-Small Cell Lung Cancer(NSCLC), Colorectal Cancer (CRC) and other solid tumors. | ||
| E1829New | Calderasib (MK-1084) | Calderasib (MK-1084) is a selective KRAS G12C inhibitor demonstrating antitumor efficacy. It can be utilized as monotherapy or in combination with pembrolizumab () for oncology research. | ||
| E2540New | Salvianolic acid F | サルビアノール酸FはKRAS阻害剤であり、特にKRAS G12Dに対して有効です。サルビアノール酸Fは同時にNF-κB、MMP-9、およびNOを阻害します。サルビアノール酸Fは、in vitroでEP300/PI3K/AKT経路を介して癌細胞の増殖、浸潤、および遊走を阻害し、アポトーシスを誘導します。サルビアノール酸Fは、in vivoでPI3K/AKTシグナル伝達経路を介してKRAS依存性肺癌細胞の増殖を阻害します。サルビアノール酸Fは、KRAS G12Dによって駆動される非小細胞肺癌（NSCLC）や卵巣癌を含む様々な癌の研究に使用できます。 | ||
| E1856 | ARS-1323 | ARS-1323 is the racemic mixture, containing ARS-1620, and a potent inhibitor of mutant KRAS G12C. It can be used in research for biochemical binding screens as companion imaging drugs (CID) for KRAS G12C. | ||
| E6643New | SS-3091 | SS - 3091はパンKRas阻害剤です。SS - 3091はKRasの相互作用界面に結合し、ARaf/KRas複合体を不安定化させ、それにより下流のシグナル伝達に影響を与えます。SS - 3091は、様々な癌細胞におけるKRas G12D、G12C、G12V、およびG12S変異体に対して有意な抗癌および抗増殖活性を有します。 | ||
| E1071 | ASP2453 | ASP2453, a potent, selective and covalent KRAS G12C inhibitor, inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf. ASP2453 is a potential therapeutic agent for KRAS G12C-mutated cancer. | ||
| E6526New | MCB-294 | MCB - 294は、NRASおよびHRASよりも選択的にKRASを阻害する二状態型パンKRAS阻害剤です。MCB - 294は、KRASの活性型（GTP結合型）と不活性型（GDP結合型）の両方に結合することができ、それぞれの解離定数（Kd）は約1 pMと10 nMです。MCB - 294は、G12D、G12C、G12V、G12S、G13Dおよび野生型KRASを発現するhTERT - HPNE細胞の増殖を広範囲に阻害し、IC50は約700 nMです。MCB - 294は、KRAS変異腫瘍において不可逆的なアポトーシスを誘導します。MCB - 294は、KRASG12C阻害剤耐性癌細胞を効果的に抑制し、腫瘍免疫微小環境を改変します。MCB - 294は、膵臓癌、結腸直腸癌および肺癌の研究に使用することができます。 | ||
| E6411New | RP03707 | RP03707は、PROTACベースのKRASG12D分解剤です（赤色：KRASG12D阻害剤 (HY - 134813)、黒色：リンカー、青色：E3リガーゼリガンド）。 | ||
| E5847New | olomorasib | Olomorasib (KRAS G12C inhibitor 19, LY3537982) is a potent and highly selective second-generation inhibitor of GDP-bound KRAS G12C, with the potential to treat patients with advanced solid tumors carrying the KRAS G12C mutation. | ||
| E6638New | VS-7375 (GFH375) | VS-7375 (GFH375) is an oral small-molecule inhibitor that selectively targets KRAS G12D in both its active (GTP-bound) and inactive (GDP-bound) forms. This dual-state inhibition results in stronger tumor suppression compared to single-state inhibitors. It exhibits potent anti-proliferative and anti-tumor effects in KRAS G12D-mutant models, including an intracranial GP2D tumor model. | ||
| E1968New | BBO-8520 | BBO-8520 is a covalent small molecule inhibitor that selectively targets KRAS G12C with high oral bioavailability. It functions as both a KRAS G12C (OFF) inhibitor and a blocker of KRAS G12C (ON) signaling. The compound inhibits cellular proliferation by binding to GTP-bound KRAS G12C (ON), thereby preventing RAS-RAF1 interaction and promoting the transition to the inactive (OFF) state . | ||
| E1157 | Pan-RAS-IN-1 | Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins. | ||
| E1962 | Zoldonrasib (RMC-9805) | Zoldonrasib (RMC-9805) is an orally active inhibitor of KRAS G12D. RMC-9805 inhibits RAS signaling, leading to apoptosis in cancer cells with the KRAS G12D mutation. | ||
| S8831 | MRTX-1257 | MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. | ||
| E1564 | BI-2493 | BI-2493, a structural analogue of BI-2865, is a highly selective inhibitor of pan-KRAS. BI-2493 attenuates tumor growth and can be used for cancer research. | ||
| E5910New | KRAS-533 | KRAS-533 is a potent agonist of KRAS that binds to the GTP/GDP-binding pocket and prevents the hydrolysis of GTP, leading to accumulation of active GTP-bound KRAS. This triggers both apoptotic and autophagic cell death pathways in cancer cells, leading to potent suppression of mutant KRAS lung cancer in vitro and in animal models. | ||
| E8295New | LY3499446 | LY3499446 (KRASG12C IN-13) is a potent inhibitor of KRAS G12C. It can be used in research on advanced solid tumors, including non-small cell lung cancer (NSCLC) and colorectal cancer (CRC). | ||
| E4758New | ACBI3 | ACBI3 is a selective and potent PROTAC degrader of pan-KRAS that promotes VHL engagement, ternary complex formation, and E3 ligase-dependent KRAS degradation with high proteome-wide selectivity. It demonstrates strong anti-tumor activity, resulting in durable pathway modulation and tumor regressions in KRAS driven cancers. | ||
| E6405New | AZD0022 | AZD0022 is a potent, orally bioavailable, selective, reversible inhibitor of KRASG12D that drives robust pathway inhibition and anti-tumour activity in KRASG12D models. | ||
| E6406New | AMG 410 | AMG410 is a non-covalent, selective inhibitor of pan-KRAS with IC50 of 1–4 nM for KRAS G12D, G12V, and G13D. It binds both GDP- and GTP-bound KRAS with Kd of 1 nM and 22 nM, respectively. AMG410 inhibits KRAS signaling in a nucleotide cycling-independent manner. It also suppresses proliferation in KRAS-amplified wild-type tumor cells. | ||
| E1959New | RMC-4998 | RMC-4998 is a tri-complex inhibitor that selectively targets the GTP-bound state of mutant KRASG12C, with high potency for KRASG12C-CYPA tri-complex formation with an IC50 of 28 nM. It strongly inhibits ERK signaling with an IC50 of 1–10 nM and attenuates AKT/MTOR and RAL pathways, leading to potent suppression of KRASG12C-driven tumor growth and can used in cancer research. | ||
| E1843New | Fulzerasib | Fulzerasib (IBI351, GFH925) is an irreversible small molecule inhibitor for KRAS G12C mutation blocking KRAS pathway signaling pERK with an IC50 of 37 nM. It demonstrates potent anti-tumor activity in multiple KRAS G12C-mutant tumor models including human pancreatic cancer, human lung adenocarcinoma, colorectal adenocarcinoma, and lung cancer models. | ||
| E1576New | LUNA18 | LUNA18 (Paluratide) is an orally bioavailable 11-mer cyclic peptide KRAS inhibitor for the intracellular tough target RAS. It binds to KRASG12D with a kd of 0.043 nM and blocks KRASG12D–SOS1 interaction at IC50 of < 2.2 nM. It also exhibits antiproliferative activity in KRAS-mutant cancer cell lines with an IC50 of 1.4 nM in AsPC-1 pancreatic cancer cells. | ||
| E1829New | Calderasib (MK-1084) | Calderasib (MK-1084) is a selective KRAS G12C inhibitor demonstrating antitumor efficacy. It can be utilized as monotherapy or in combination with pembrolizumab () for oncology research. | ||
| E2540New | Salvianolic acid F | サルビアノール酸FはKRAS阻害剤であり、特にKRAS G12Dに対して有効です。サルビアノール酸Fは同時にNF-κB、MMP-9、およびNOを阻害します。サルビアノール酸Fは、in vitroでEP300/PI3K/AKT経路を介して癌細胞の増殖、浸潤、および遊走を阻害し、アポトーシスを誘導します。サルビアノール酸Fは、in vivoでPI3K/AKTシグナル伝達経路を介してKRAS依存性肺癌細胞の増殖を阻害します。サルビアノール酸Fは、KRAS G12Dによって駆動される非小細胞肺癌（NSCLC）や卵巣癌を含む様々な癌の研究に使用できます。 | ||
| E6643New | SS-3091 | SS - 3091はパンKRas阻害剤です。SS - 3091はKRasの相互作用界面に結合し、ARaf/KRas複合体を不安定化させ、それにより下流のシグナル伝達に影響を与えます。SS - 3091は、様々な癌細胞におけるKRas G12D、G12C、G12V、およびG12S変異体に対して有意な抗癌および抗増殖活性を有します。 | ||
| E6526New | MCB-294 | MCB - 294は、NRASおよびHRASよりも選択的にKRASを阻害する二状態型パンKRAS阻害剤です。MCB - 294は、KRASの活性型（GTP結合型）と不活性型（GDP結合型）の両方に結合することができ、それぞれの解離定数（Kd）は約1 pMと10 nMです。MCB - 294は、G12D、G12C、G12V、G12S、G13Dおよび野生型KRASを発現するhTERT - HPNE細胞の増殖を広範囲に阻害し、IC50は約700 nMです。MCB - 294は、KRAS変異腫瘍において不可逆的なアポトーシスを誘導します。MCB - 294は、KRASG12C阻害剤耐性癌細胞を効果的に抑制し、腫瘍免疫微小環境を改変します。MCB - 294は、膵臓癌、結腸直腸癌および肺癌の研究に使用することができます。 | ||
| E6411New | RP03707 | RP03707は、PROTACベースのKRASG12D分解剤です（赤色：KRASG12D阻害剤 (HY - 134813)、黒色：リンカー、青色：E3リガーゼリガンド）。 | ||
| E5847New | olomorasib | Olomorasib (KRAS G12C inhibitor 19, LY3537982) is a potent and highly selective second-generation inhibitor of GDP-bound KRAS G12C, with the potential to treat patients with advanced solid tumors carrying the KRAS G12C mutation. | ||
| E6638New | VS-7375 (GFH375) | VS-7375 (GFH375) is an oral small-molecule inhibitor that selectively targets KRAS G12D in both its active (GTP-bound) and inactive (GDP-bound) forms. This dual-state inhibition results in stronger tumor suppression compared to single-state inhibitors. It exhibits potent anti-proliferative and anti-tumor effects in KRAS G12D-mutant models, including an intracranial GP2D tumor model. | ||
| E1968New | BBO-8520 | BBO-8520 is a covalent small molecule inhibitor that selectively targets KRAS G12C with high oral bioavailability. It functions as both a KRAS G12C (OFF) inhibitor and a blocker of KRAS G12C (ON) signaling. The compound inhibits cellular proliferation by binding to GTP-bound KRAS G12C (ON), thereby preventing RAS-RAF1 interaction and promoting the transition to the inactive (OFF) state . | ||
| E5910New | KRAS-533 | KRAS-533 is a potent agonist of KRAS that binds to the GTP/GDP-binding pocket and prevents the hydrolysis of GTP, leading to accumulation of active GTP-bound KRAS. This triggers both apoptotic and autophagic cell death pathways in cancer cells, leading to potent suppression of mutant KRAS lung cancer in vitro and in animal models. | ||
| E5910New | KRAS-533 | KRAS-533 is a potent agonist of KRAS that binds to the GTP/GDP-binding pocket and prevents the hydrolysis of GTP, leading to accumulation of active GTP-bound KRAS. This triggers both apoptotic and autophagic cell death pathways in cancer cells, leading to potent suppression of mutant KRAS lung cancer in vitro and in animal models. |
KRasシグナル伝達経路
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