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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-BLU-222
BLU-222

Chemical Structure : BLU-222

CAS No.: 2888704-84-3

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BLU-222 (Cirtociclib, BLU222)

货号: PC-23995Not For Human Use, Lab Use Only.

Cirtociclib (BLU-222) is a potent, highly selective, ATP-competitive CDK2 inhibitor with IC50 of 2.6 nM (CDK2/cyclinE1) with strong selectivity (>200-fold) over CDK family members (1/4/6/7/9).

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10 mg ￥3580 In stock
25 mg ￥5880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Cirtociclib (BLU-222) is a potent, highly selective, ATP-competitive CDK2 inhibitor with IC50 of 2.6 nM (CDK2/cyclinE1) with strong selectivity (>200-fold) over CDK family members (1/4/6/7/9).
BLU-222 has excellent kinome selectivity with an S(10) of 0.045, measured by KINOMEscan at 3 µM.
BLU-222 displays nanomolar cellular potency on phosphorylated Rb (pRb) T821/826 with strong selectivity over pLamin S22, a measure of CDK1 activity in CDK2-dependent cell line OVCAR-3.
BLU-222 displays nanomolar cellular potency on phosphorylated Rb (pRb) T821/826 with strong selectivity over pLamin S22, a measure of CDK1 activity. BLU-222 potently and dose-dependently inhibited proliferation in CCNE1amplified ovarian/endometrial cancer cell lines, while sparing CCNE1-normal (diploid, mRNA not overexpressed) cell lines.
BLU-222 disrupts Rb signaling in CCNE1-amplified cells to arrest cell cycle progression. BLU-222 demonstrated robust activity in combination with carboplatin or paclitaxel in CCNE1-aberrant models, rendering chemotherapy-resistant tumors strongly sensitive to the combination.

物理化学性质&存储条件

分子量 365.34
分子式 C15H17F2N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(5-(difluoromethoxy)-1H-pyrazol-3-yl)-1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-pyrazolo[3,4-b]pyrazin-6-amine

参考文献

1. Dommer AP, et al. Cancer Res. 2025 Feb 13. doi: 10.1158/0008-5472.CAN-24-2244.

2. House NC, et al. Cancer Res. 2025 Feb 13. doi: 10.1158/0008-5472.CAN-24-2360.

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