294646-77-8
294646-77-8 結(jié)構(gòu)式
基本信息
(S)-CR8
(R)-CR8
CR8, (R)-Isomer
CR8, (R)-Isomer - CAS 294646-77-8 - Calbiochem
(R)-2-(1-Hydroxybut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine
2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-(4-(2-pyridyl)benzyl)-9-isopropylpurinetrihydrochloride
(2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-butanol-1
(2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-1-butanol
1-Butanol,2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]Methyl]aMino]-9H-purin-2-yl]aMino]-,(2R)-
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2025/02/08 | HY-18340 | (2R)-2-[[9-異丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇 (R)?-?CR8 | 294646-77-8 | 5mg | 2500元 |
| 2025/02/08 | HY-18340 | (2R)-2-[[9-異丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇 (R)?-?CR8 | 294646-77-8 | 10 mM * 1 mLin DMSO | 2750元 |
| 2025/02/08 | HY-18340 | (2R)-2-[[9-異丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇 (R)?-?CR8 | 294646-77-8 | 10mg | 4000元 |
常見問(wèn)題列表
|
Cdk1/cyclin B 0.09 μM (IC 50 ) |
cdk2/cyclin A 0.072 μM (IC 50 ) |
CDK2/cyclinE 0.041 μM (IC 50 ) |
Cdk5/p25 0.11 μM (IC 50 ) |
CDK7/cyclin H 1.1 μM (IC 50 ) |
CDK9/Cyclin T 0.18 μM (IC 50 ) |
CK1δ/ε 0.4 μM (IC 50 ) |
(R)-CR8 (CR8) (0.1-100 μM; 48 hours) is a potent inducer of apoptotic cell death with an IC
50
of 0.49 μM for SH-SY5Y cell line.
(R)-CR8 (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage.
The CDK-bound form of (R)-CR8 has a solvent-exposed pyridyl moiety that induces the formation of a complex between CDK12-cyclin K and the CUL4 adaptor protein DDB1, bypassing the requirement for a substrate receptor and presenting cyclin K for ubiquitination and degradation.
Apoptosis Analysis
| Cell Line: | SH-SY5Y cell line |
| Concentration: | 0.1, 1, 10, 100 μM |
| Incubation Time: | 24 hours |
| Result: | Reduced cell survival in a dose-dependent manner. |
(R)-CR8 (5?mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment.
| Animal Model: | Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330?g) |
| Dosage: | i.p. |
| Administration: | 5?mg/Kg |
| Result: | Resulted in a significant reduction in lesion size. |