2152628-33-4
LOXO-292
CAS: 2152628-33-4
Molecular Formula: C₂₉H₃₁N₇O₃
2152628-33-4 - Names and Identifiers
2152628-33-4 - Physico-chemical Properties
| Molecular Formula | C₂₉H₃₁N₇O₃ |
| Molar Mass | 525.60 |
| Density | 1.36±0.1 g/cm3(Predicted) |
| Solubility | DMSO : 20.83 mg/mL (39.63 mM; Need ultrasonic) |
| pKa | 14.00±0.29(Predicted) |
| Storage Condition | -20℃ |
| Physical and Chemical Properties | Bioactive Selpercatinib (LOXO-292, ARRY-192) is an effective and specific RET (c-RET) inhibitor for WT RET (c-RET), RET (c-RET) (V804M), RET (c-RET) (V804L), RET (c-RET) (A883F), the IC50 values of RET (c-RET) (M918T) and RET (c-RET) (S891A) are 1 nM, 2 nM, 2 nmM, 4 nM, 2 nM and 2 nM respectively. |
| Use | Role sekatinib is a potent Src inhibitor with an IC50 of 2.7 nM, and is also effective in c-Yes, Fyn, Lyn, Blk, Fgr and Lck. The activity of acting on Abl and EGFR (L858R and L861Q) is slightly lower. Secatinib is the first inhibitor of the Src pathway in human tumor tissue. |
2152628-33-4 - Reference
| Reference Show more | 1: Russo A, Lopes AR, McCusker MG, Garrigues SG, Ricciardi GR, Arensmeyer KE, Scilla KA, Mehra R, Rolfo C. New Targets in Lung Cancer (Excluding EGFR, ALK, ROS1). Curr Oncol Rep. 2020 Apr 16;22(5):48. doi: 10.1007/s11912-020-00909-8. PMID: 32296961. 2: Dias-Santagata D, Lennerz JK, Sadow PM, Frazier RP, Govinda Raju S, Henry D, Chung T, Kherani J, Rothenberg SM, Wirth LJ. Response to RET-Specific Therapy in RET Fusion-Positive Anaplastic Thyroid Carcinoma. Thyroid. 2020 Apr 15. doi: 10.1089/thy.2019.0477. Epub ahead of print. PMID: 32292131. 3: Zhao Z, Fu T, Gao J, Xu Y, Wu X, Chen W, Li X, Yu R, Shao YW, Li M, Yao Y. Identifying novel oncogenic RET mutations and characterising their sensitivity to RET-specific inhibitors. J Med Genet. 2020 Apr 13:jmedgenet-2019-106546. doi: 10.1136/jmedgenet-2019-106546. Epub ahead of print. PMID: 32284345. 4: Solomon BJ, Tan L, Lin JJ, Wong SQ, Hollizeck S, Ebata K, Tuch BB, Yoda S, Gainor JF, Sequist LV, Oxnard GR, Gautschi O, Drilon A, Subbiah V, Khoo C, Zhu EY, Nguyen M, Henry D, Condroski KR, Kolakowski GR, Gomez E, Ballard J, Metcalf AT, Blake JF, Dawson SJ, Blosser W, Stancato LF, Brandhuber BJ, Andrews S, Robinson BG, Rothenberg SM. RET Solvent Front Mutations Mediate Acquired Resistance to Selective RET Inhibition in RET-Driven Malignancies. J Thorac Oncol. 2020 Apr;15(4):541-549. doi: 10.1016/j.jtho.2020.01.006. Epub 2020 Jan 24. PMID: 31988000. 5: Tiedje V, Fagin JA. Therapeutic breakthroughs for metastatic thyroid cancer. Nat Rev Endocrinol. |
2152628-33-4 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.903 ml | 9.513 ml | 19.026 ml |
| 5 mM | 0.381 ml | 1.903 ml | 3.805 ml |
| 10 mM | 0.19 ml | 0.951 ml | 1.903 ml |
| 5 mM | 0.038 ml | 0.19 ml | 0.381 ml |
Last Update：2024-01-02 23:10:35
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