Sunitinib

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。

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。

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。

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。

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).

Sunitinib-d4 是 Sunitinib 的氘代化合物。

N-Desethyl Sunitinib hydrochloride (SU-12662 hydrochloride) 是 Sunitinib 的活性代谢物，具有潜在的抗癌活性，可用于研究癌症。

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。

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。

Elacridar (GG918) 是一种有效的 P-糖蛋白和BCRP 的抑制剂。

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 to Sunitinib and Erlotinib and that Vps34 is a promising therapeutic target for combination strategies in breast cancer.

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.