化合物 T30600
|
|
|
- CAS號(hào):
- 2349356-09-6
- 英文名:
- BSJ-03-204
- 英文別名:
- BSJ-03-204;N-[4-[4-[6-[(6-Acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]butyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetamide;Acetamide, N-[4-[4-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]butyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-
- 中文名:
- 化合物 T30600
- 中文別名:
- 化合物 T30600;化合物 BSJ-03-204;N-[4-[4-[6-[(6-乙?；?8-環(huán)戊基-7,8-二氫-5-甲基-7-氧代吡啶并[2,3-D]嘧啶-2-基)氨基]-3-吡啶基]-1-哌嗪基]丁基]-2-[[2-(2,6-二氧代-3-哌啶基)-2,3-二氫-1,3-二氧代-1H-異吲哚-4-基]氧基]乙酰胺
- CBNumber:
- CB85985157
- 分子式:
- C43H48N10O8
- 分子量:
- 832.9
- MOL File:
- 2349356-09-6.mol
|
|
|
化合物 T30600化學(xué)性質(zhì)
-
密度:
-
1.397±0.06 g/cm3(Predicted)
-
|
-
儲(chǔ)存條件:
-
-20°C, protect from light
-
|
-
溶解度:
-
Soluble in DMSO
-
|
-
形態(tài):
-
Solid
-
|
-
酸度系數(shù)(pKa):
-
10.68±0.40(Predicted)
-
|
-
顏色:
-
Light yellow to green yellow
-
|
化合物 T30600性質(zhì)、用途與生產(chǎn)工藝
BSJ-03-204 是一種有效的，選擇性的基于 Palbociclib (HY-50767) 的 CDK4/6 雙重降解劑 (PROTAC)，對(duì) CDK4/D1 和 CDK6/D1 的 IC50 分別為 26.9 nM 和 10.4 nM。BSJ-03-204 不誘導(dǎo) IKZF1/3 降解，具有抗癌活性。
|
CDK4/D1
26.9 nM (IC
50
)
|
CDK6/D1
10.4 nM (IC
50
)
|
BSJ-03-204 (0.0001-100 μM; for 3 or 4 days) has potent anti-proliferative effects on MCL cell lines.
BSJ-03-204 (1 μM; for 1 day) potently induces a G1 arrest.
BSJ-03-204 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4/6 in WT cells, not IKZF1/3.
Cell Proliferation Assay
|
Cell Line:
|
MCL cell lines (Jeko-1, Mino, Granta-519, Rec-1, and Maver-1 cells)
|
|
Concentration:
|
0.0001-100 μM
|
|
Incubation Time:
|
For 3 or 4 days
|
|
Result:
|
Had potent anti-proliferative effects on mantle cell lymphoma (MCL) cell lines.
|
Cell Cycle Analysis
|
Cell Line:
|
Granta-519 cells
|
|
Concentration:
|
1 μM
|
|
Incubation Time:
|
For 1 day
|
|
Result:
|
Potently induced a G1 arrest.
|
Western Blot Analysis
|
Cell Line:
|
Wildtype (WT) or Crbn
-/-
Jurkat cells
|
|
Concentration:
|
0.1, 0.5, 1, 5 μM
|
|
Incubation Time:
|
For 4 hours
|
|
Result:
|
Only resulted in degradation of CDK4/6 in WT cells, not IKZF1/3.
|
化合物 T30600
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS編號(hào) | 包裝 | 價(jià)格 |
|---|
| 2026/06/05 | HY-136250 | 化合物 T30600
BSJ-03-204 | 2349356-09-6 | 1 mg | 1591元 |
| 2026/06/05 | HY-136250 | 化合物 T30600
BSJ-03-204 | 2349356-09-6 | 5mg | 3500元 |
2349356-09-6, 化合物 T30600 相關(guān)搜索:
- 抑制劑
- C43H48N10O8
- 化合物 BSJ-03-204
- N-[4-[4-[6-[(6-乙?；?8-環(huán)戊基-7,8-二氫-5-甲基-7-氧代吡啶并[2,3-D]嘧啶-2-基)氨基]-3-吡啶基]-1-哌嗪基]丁基]-2-[[2-(2,6-二氧代-3-哌啶基)-2,3-二氫-1,3-二氧代-1H-異吲哚-4-基]氧基]乙酰胺
- 化合物 T30600
- 2349356-09-6
- N-[4-[4-[6-[(6-Acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]butyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetamide
- Acetamide, N-[4-[4-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]butyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-
- BSJ-03-204