SML1932

A-1210477

≥98% (HPLC)

• 동의어(들): 7-(1,3-Dimethyl-5-((4-(4-(methylsulfonyl)piperazin-1-yl)phenoxy)methyl)-1H-pyrazol-4-yl)-1-(2-morpholinoethyl)-3-(3-(naphthalen-1-yloxy)propyl)-1H-indole-2-carboxylic acid, 7-[5-[[4-[4-[(Dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-1H-indole-2-carboxylic acid
• 실험식(Hill 표기법): C₄₆H₅₅N₇O₇S
• CAS Number: 1668553-26-1
• Molecular Weight: 850.04
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: powder
• 색상: white to beige
• solubility: DMSO: 2 mg/mL, clear
• 저장 온도: −20°C
• SMILES string: O=C(O)C(N1CCN2CCOCC2)=C(C3=C1C(C4=C(N(N=C4C)C)COC5=CC=C(C=C5)N6CCN(CC6)S(=O)(N(C)C)=O)=CC=C3)CCCOC7=C8C=CC=CC8=CC=C7.[H]Cl
• InChI key: MRLDHNSBXWSDDL-UHFFFAOYSA-N

설명

생화학적/생리학적 작용

A BH3 mimetic that targets MCL-1 with high affinity and selectivity. Selectively inhibits cancer survival in a MCL-1-dependent manner.

A-1210477 is a BH3 mimetic that targets MCL-1 with high affinity (Ki = 0.43 nM) and selectivity (Ki >0.66 μM for BCL-2, BCL-XL, BCL-W, and A1), exhibiting little to no activity toward panels of 80 kinases (IC50 >8.5 μM) and 21 GPCRs (IC50 & EC50 >10 μM). A-1210477 selectively inhibits the survival of MCL-1-dependent (IC50 ~4 μM/multiple myeloma H929, 5.3 μM/NSCLC H2110, 7.2 μM/NSCLC H23), but not BCL-2-dependent RS4;11, cultures via apoptosis induction and potentiates BCL-2/BCL-XL inhibitor ABT-263 (Navitoclax) killing in a variety of cancer cell cultures where ABT-263 alone is ineffective. A-1210477 is also shown to cause cellular MCL-1 upregulation, most likely due to blocking MCL-1 interaction with BH3-only proteins such as NOXA and MULE known to mediate MCL-1 ubiquitylation for proteasomal degradation.

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable