| DC70846 |
TH-Z835 |
TH-Z835 is a potent, mutant selective KRAS (G12D) inhibitor with IC50 of 1.6 uM.TH-Z835 binds to both GDP-bound and GMPPNP-bound KRAS G12D with similar affinities, efficiently disrupt KRAS–CRAF interaction, but do not bind to wide type and G12C mutant KRAS.TH-Z835 reduced the pERK level in PANC-1 cells with an IC50 <2.5 uM, exhibited anti-proliferative effects for KRAS(G12D)-bearing pancreatic cancer cell lines PANC-1 and KPC with IC50 of <0.5 uM, induced arrest at the G1 phase of the cell cycle.TH-Z835 displayed anti-tumor effects alone and in combination with anti-PD-L1 antibody in xenograft pancreatic tumor models. |
|
| DC70899 |
VUBI1 |
VUBI1 is a potent activator of SOS1 which modulates the KRAS pathway, binds directly to SOS1 (Kd=44 nM);
VUBI1 increase nucleotide exchange on RAS in vitro at sub-micromolar concentration, rapidly enhances cellular RAS-GTP levels, and invoke biphasic signaling changes in phosphorylation of ERK 1/2 (Hela pERK ICW EC50=5.9 uM). |
|
| DC71619 |
GDC-6036-NH |
GDC-6036-NH is from patent WO2020097537A2, and a precursor of compound 17 a/b. Compound 17 a/b is a RAS inhibitor and can be used in cancer research. |
|
| DC71620 |
MRTX-EX185 formic |
MRTX-EX185 formic is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 formic also binds GDP-loaded HRAS. |
|
| DC71621 |
(Rac)-Antineoplaston A10 |
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10, which is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer. |
|
| DC71911 |
G12Si-1 |
G12Si-1 is a selective K-Ras(G12S) covalent inhibitor, which can inhibit oncogenic signaling of K-Ras(G12S). G12Si-1 shows good ability to covalently engage recombinant K-Ras(G12S) at the mutant serine residue. G12Si-1 can also affect nucleotide cycling of K-Ras by blocking Sos-catalyzed exchange and decreasing the rate of EDTA promoted exchange. |
|
| DC71912 |
G12Si-2 |
G12Si-2, an analog of G12Si-1, is a negative control tool. G12Si-2 is not a covalent inhibitor of the G12C mutant of K-Ras. |
|
| DC72237 |
BI-0474
Featured
|
BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models. |
|
| DC72491 |
ZG1077 |
ZG1077 is a covalent KRAS G12C inhibitor. ZG1077 can be used in the research of non-small cell lung cancer (NSCLC). |
|
| DC72743 |
Spiclomazine hydrochloride |
Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis. |
|
| DC72744 |
(S)-JDQ-443 |
(S)-JDQ-443 is an isomer of JDQ-443. JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity. |
|
| DC72745 |
ARS-2102 |
ARS-2102 is a potent covalent KRAS G12C inhibitor for use in cancer research. |
|
| DC74353 |
1-AM |
A potent, selective, covalent KRAS G12C inhibitor that selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations.. |
|
| DC74354 |
6H05 trifluoroacetate |
6H05 is a selective, allosteric inhibitor of oncogenic mutant K-Ras(G12C), an intermediate for the synthesis of other oncogenic K-Ras(G12C) inhibitors.. |
|
| DC74355 |
ACA-14 |
ACA-14 is a small molecule direct inhibitor of KRAS, impedes the interaction of KRAS with its effector Raf and reduces both intrinsic and SOS-mediated nucleotide exchange rates. |
|
| DC74356 |
ACA22 |
ACA22 is a small molecule KRAS inhibitor, inhibits KRAS-mediated signal transduction in cells expressing wild type (WT) and G12D mutant KRAS. |
|
| DC74357 |
ADT-007 |
ADT-007 (ADT007) is a potent, specific pan-RAS inhibitor, shows potential to circumvent resistance to mutant-specific KRAS inhibitors and activates antitumor immunity. |
|
| DC74358 |
ASP6918 |
ASP6918 (ASP 6918) is a highly potent, covalent KRAS G12C inhibitor with IC50 of 28 nM in cell-free assays, and pERK inhibition IC50 of 3.7 nM in NCI-H1373 cells. |
|
| DC74359 |
BBO-8956 |
BBO-8956 is a highly potent, covalent inhibitor of GTP-KRAS G12C, BBO-8956 is effective against both GDP and GTP-bound KRAS G12C. |
|
| DC74360 |
BC-DXI-32982
Featured
|
BC-DXI-32982 is a potent inhibitor of the interaction between DX2 and KRAS4B with a half-maximal inhibitory concentration (IC50) of 0.18 μM, showing little effect on the PRKACA-PRKAR2A interaction. |
|
| DC74361 |
CSC01 |
CSC01 is a small molecule inhibitor of oncogenic KRAS mutant G13D (KRAS-G13D). |
|
| DC74362 |
ERAS-5024 |
ERAS-5024 (ERAS5024) is a potent and selective KRAS G12D inhibitor with IC50 of 0.86 nM in RAS-RAF binding assays, inhibits ERK1/2 phosphorylation (pERK) formation with IC50 of 2.1 nM in AsPC-1 cell-based assays. |
|
| DC74363 |
Fulzerasib |
Fulzerasib is a potent selective inhibitor of KRAS gene mutation. |
|
| DC74364 |
G12Si-5 |
G12Si-5 is a specific small molecule that covalently target K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM. |
|
| DC74365 |
RMC-4998
Featured
|
RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM. |
|
| DC74366 |
RSC-1255 |
RSC-1255 (KRAS inhibitor 249C, V-ATPase inhibitor) is a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancer cells (A549 (KRASG12S), IC50=73 nM), binds to V-ATPase (Kd=23 nM) and inhibits its activity. |
|
| DC74367 |
SCH53239 |
SCH-53239 (SCH53239) is a small molecule inhibitor of Ras nucleotide exchange with IC50 of 0.5 uM, bind competitively with GDP in the nucleotide binding site of the Ras protein. |
|
| DC74368 |
SIJ1772 |
SIJ1772 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 77 and 96 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively. |
|
| DC74369 |
SIJ1795 |
SIJ1795 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 82 and 75 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively. |
|
| DC74574 |
LY3537982 (KRAS G12C inhibitor 19) |
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. |
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