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847871-99-2

中文名稱(chēng) 來(lái)那度胺半水合物
英文名稱(chēng) LenalidoMide (heMihydrate)
CAS 847871-99-2
分子式 C26H28N6O7
分子量 536.537
MOL 文件 847871-99-2.mol
更新日期 2025/01/13 16:39:38
847871-99-2 結(jié)構(gòu)式 847871-99-2 結(jié)構(gòu)式

基本信息

中文別名
來(lái)那度胺半水合物
TNF-Α分泌抑制劑
英文別名
CC-5013 hemihydrate
LenalidoMide (heMihydrate)
所屬類(lèi)別
有機(jī)原料:氨基化合物

物理化學(xué)性質(zhì)

儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO : 50 mg/mL (186.38 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
形態(tài)粉末
顏色Off-white to pink
InChIInChI=1S/2C13H13N3O3.H2O/c2*14-9-3-1-2-7-8(9)6-16(13(7)19)10-4-5-11(17)15-12(10)18;/h2*1-3,10H,4-6,14H2,(H,15,17,18);1H2
InChIKeyOTJHSDXKMBRCMM-UHFFFAOYSA-N
SMILESO=C1C2C([H])=C([H])C([H])=C(C=2C([H])([H])N1C1([H])C(N([H])C(C([H])([H])C1([H])[H])=O)=O)N([H])[H].O=C1C2C([H])=C([H])C([H])=C(C=2C([H])([H])N1C1([H])C(N([H])C(C([H])([H])C1([H])[H])=O)=O)N([H])[H].O([H])[H]

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P305+P351+P338
來(lái)那度胺半水合物價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-A0003B來(lái)那度胺半水合物
Lenalidomide hemihydrate
847871-99-2100 mg1350元
2024/11/08HY-A0003B來(lái)那度胺半水合物
Lenalidomide hemihydrate
847871-99-210mM * 1mLin DMSO1485元
2024/11/08HY-A0003B來(lái)那度胺半水合物
Lenalidomide hemihydrate
847871-99-2500mg2200元

常見(jiàn)問(wèn)題列表

生物活性
Lenalidomide hemihydrate (CC-5013 hemihydrate) 是 Thalidomide 的衍生物,也是一種具有口服活性免疫調(diào)節(jié)劑。Lenalidomide hemihydrate (CC-5013 hemihydrate) 是一種泛素 E3 連接酶 cereblon (CRBN) 的配體,通過(guò) CRBN-CRL4 泛素連接酶對(duì)兩種淋巴轉(zhuǎn)錄因子 IKZF1 和 IKZF3 進(jìn)行選擇性泛素化和降解。Lenalidomide hemihydrate (CC-5013 hemihydrate) 特別地抑制成熟 B 細(xì)胞淋巴瘤 (包括多發(fā)性骨髓瘤) 的生長(zhǎng),并誘導(dǎo) T 細(xì)胞釋放白細(xì)胞介素-2 (IL-2)。
靶點(diǎn)

Cereblon

體外研究

Lenalidomide is potent in stimulating T cell proliferation and IFN-γ and IL-2 production. Lenalidomide has been shown to inhibit production of pro inflammatory cytokines TNF-α, IL-1, IL-6, IL-12 and elevate the production of anti-inflammatory cytokine IL-10 from human PBMCs. Lenalidomide downregulates the production of IL-6 directly and also by inhibiting multiple myeloma (MM) cells and bone marrow stromal cells (BMSC) interaction, which augments the apoptosis of myeloma cells. Dose-dependent interaction with the CRBN-DDB1 complex is observed with Thalidomide, Lenalidomide and Pomalidomide, with IC 50 values of ~30?μM, ~3?μM and ~3?μM, respectively, These reduced CRBN expression cells (U266-CRBN 60 and U266-CRBN 75 ) are less responsive than the parental cells to antiproliferative effects Lenalidomide across a dose-response range of 0.01 to 10?μM. Lenalidomide, a thalidomide analog, functions as a molecular glue between the human E3 ubiquitin ligase cereblon and CKIα is shown to induce the ubiquitination and degradation of this kinase, thus presumably killing leukemic cells by p53 activation.

體內(nèi)研究

The toxicity of Lenalidomide doses up to 15, 22.5, and 45 mg/kg via IV, IP, and PO routes of administration. Limited by solubility in our PBS dosing vehicle, these maximum achievable Lenalidomide doses are well tolerated with the exception of one mouse death (of four total dosed) at the 15 mg/kg IV dose. Notably, no other toxicities are observed in the study at IV doses of 15 mg/kg (n=3) or 10 mg/kg (n=45) or at any other dose level through IV, IP, and PO routes.

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