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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
---|---|---|---|---|
I128086-5mg |
5mg |
现货 ![]() |
| |
I128086-25mg |
25mg |
现货 ![]() |
| |
I128086-100mg |
100mg |
现货 ![]() |
|
别名 | INK-128;MLN0128 |
---|---|
英文别名 | Sapanisertib; MLN0128; 3-(2-amino-5-benzoxazolyl)-1-(1-methylethyl)-1h-pyrazolo(3,4-d)pyrimidin-4-amine;3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine |
规格或纯度 | ≥98% |
英文名称 | INK 128 (MLN0128) |
生化机理 | INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases [1]. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inhibits AKT phosphorylation at Ser473, the downstream substrate of TORC2. Furthermore, INK 128 also shows potent inhibition effects on cell lines resistant to rapamycin and pan-PI3K inhibitors |
储存温度 | -20°C储存 |
运输条件 | 超低温冰袋运输 |
备注 | 5mg卖完停产,不再备货 |
产品介绍 |
INK 128是高活性mTOR抑制剂,IC50为1 nM,比对其它I型PI3K亚型的抑制性高200倍。A potent and selective TORC1/2 inhibitor INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). |
IUPAC Name | 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine |
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INCHI | InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19) |
InChi Key | GYLDXIAOMVERTK-UHFFFAOYSA-N |
Canonical SMILES | CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N |
PubChem CID | 45375953 |
分子量 | 309.33 |
溶解性 | DMSO |
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输入批号以搜索COA:
1. Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. (2009) mTOR Mediated Anti-Cancer Drug Discovery.. Drug Discov Today Ther Strateg, 6 (2): (47-55). [PMID:20622997] |
2. Schenone S, Brullo C, Musumeci F, Radi M, Botta M. (2011) ATP-competitive inhibitors of mTOR: an update.. Curr Med Chem, 18 (20): (2995-3014). [PMID:21651476] |
3. Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, Shi EY, Stumpf CR, Christensen C, Bonham MJ et al.. (2012) The translational landscape of mTOR signalling steers cancer initiation and metastasis.. Nature, 485 (7396): (55-61). [PMID:22367541] |
4. Arendse LB, Murithi JM, Qahash T, Pasaje CFA, Godoy LC, Dey S, Gibhard L, Ghidelli-Disse S, Drewes G, Bantscheff M et al.. (2022) The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages.. Sci Transl Med, 14 (667): (eabo7219). [PMID:36260689] |