Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T0374L |
Sunitinib
苏尼替尼,舒尼替尼,SU 11248 |
Apoptosis; Mitophagy; VEGFR; FLT; IRE1; PDGFR; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors |
Sunitinib (SU 11248) 是一种多靶点受体酪氨酸激酶 (RTK) 抑制剂,可以抑制 VEGFR2 和 PDGFRβ (IC50=80/2 nM)。Sunitinib 具有抗肿瘤活性,可以用于治疗肾癌和胃肠道肿瘤。 | |||
T0374 |
Sunitinib Malate
苏尼替尼苹果酸盐,Sutent,SU 11248 (Malate),SU 11248,Sunitinib |
Apoptosis; Mitophagy; VEGFR; FLT; IRE1; PDGFR; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors |
Sunitinib Malate (Sunitinib) 是一种基于吲哚酮的酪氨酸激酶抑制剂,抑制 VEGFR2和 PDGFRβ的 IC50分别为80 nM 和 2 nM。它是 ATP 竞争性抑制剂,可通过抑制自身磷酸化和随后的 RNase 激活来有效抑制 Ire1α的磷酸化。 | |||
T60128 |
N,N-Didesethyl Sunitinib Hydrochloride
|
AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
N,N-Didesethyl Sunitinib Hydrochloride 是一种有效的AMPK 抑制剂,对AMPKα1和AMPK2的IC50分别为393nM 和141nM。 | |||
T13039 |
Sunitinib-d10
Sunitinib D10,SU 11248 D10 |
VEGFR; PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Sunitinib D10 is a deuterium labeled Sunitinib. Sunitinib is a inhibitor of multi-targeted receptor tyrosine kinase(IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively). | |||
T12145 |
N-Desethyl Sunitinib
N-去乙基-舒尼替尼,SU-11662 |
VEGFR; PDGFR; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
N-Desethyl Sunitinib (SU-11662) 是 Sunitinib 的代谢物。其中 Sunitinib 是有效的以及ATP 竞争的VEGFR、PDGFRβ和KIT 抑制剂,能够抑制 VEGFR -1 (Ki:2 nM) 、VEGFR-2 (Ki:9 nM) 、VEGFR-3 (Ki:17 nM) 、PDGFRβ (Ki:8 nM) 、KIT (Ki:4 nM) 的活性。 | |||
T74127 | N-Desethyl Sunitinib hydrochloride | ||
N-Desethyl Sunitinib (SU-12662) (hydrochloride) 是 Sunitinib 的代谢物。Sunitinib 是有效的,ATP 竞争的VEGFR,PDGFRβ和KIT 抑制剂,能够抑制VEGFR-1,VEGFR-2,VEGFR-3,PDGFRβ和 KIT 的活性,Ki 值分别为 2,9,17,8 和 4 nM。 | |||
T2657 |
Elacridar
GW0918,依克立达,GW120918,GF120918,GG918 |
BCRP; P-gp | Membrane transporter/Ion channel; Neuroscience |
Elacridar (GG918) 是一种有效的 P-糖蛋白和BCRP 的抑制剂。 | |||
T12145L |
N-Desethylsunitinib hydrochloride
|
VEGFR; PDGFR; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
N-Desethylsunitinib hydrochloride 是舒尼替尼的主要且具有药理活性的代谢物,是有效的 ATP 竞争性 VEGFR、PDGFRβ 和 KIT 抑制剂。 | |||
T9421 |
5-(5-Fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic Acid
|
Others | Others |
5-(5-Fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic Acid 为舒尼替尼杂质。 | |||
T39512 |
Thalidomide-NH-C6-NH-Boc
Thalidomide-NH-C6-NH-Boc |
||
Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate containing the cereblon ligand derived from Thalidomide and a linker utilized in the synthesis of MI-389 (compound 22). MI-389 is a highly effective phthalimide PROTAC degrader developed from the multi-targeted receptor tyrosine kinase inhibitor sunitinib. | |||
T69888 |
SB02024
|
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SB02024 is a VPS34 inhibitor. SB02024 activates cGAS-STING signaling and sensitizes tumors to STING agonist. SB02024 blocked autophagy in vitro and reduced xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7, in vivo. Vps34 inhibitor significantly potentiated cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro in monolayer cultures and when grown as multicellular spheroids. Our data suggests that inhibition of autophagy significantly improves sensitivity... |