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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Wee1-RP-6306
RP-6306

Chemical Structure : RP-6306

CAS No.: 2719793-90-3

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RP-6306 (Lunresertib, RP6306, (S)-RP-6306)

货号: PC-73399Not For Human Use, Lab Use Only.

RP-6306 (Lunresertib, RP6306) is a first-in-class, potent and selective, orally available inhibitor of PKMYT1 with IC50 of 2.4 nM, displays less potency (>35-fold) against EphA1-2, and EphB2-4, and Wee1.

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5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: 98.46% (HPLC) Select Batch:

生物&药学活性

RP-6306 (Lunresertib, RP6306) is a first-in-class, potent and selective, orally available inhibitor of PKMYT1 with IC50 of 2.4 nM, displays less potency (>35-fold) against EphA1-2, and EphB2-4, and Wee1.
RP-6306 inhibits the phosphorylation of CDK1 Thr14 in vivo in tumor tissue and inhibits CCNE1-amplified tumor cell growth in several preclinical xenograft models.
PKMYT1 is an important regulator of CDK1 phosphorylation and is a compelling therapeutic target for the treatment of certain types of DNA damage response cancers due to its established synthetic lethal relationship with CCNE1 amplification.
PKMYT1 is a member of the Wee-kinase family protein kinases, PKMYT1 is involved in G2/M checkpoint regulation of the cell cycle.

物理化学性质&存储条件

分子量 324.384
分子式 C18H20N4O2
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

(1S)-2-Amino-1-(3-hydroxy-2,6-dimethylphenyl)-5,6-dimethyl-1H-pyrrolo[2,3-b]pyridine-3-carboxamide

参考文献

1. Janek Szychowski, et al. Discovery of an orally bioavailable and selective PKMYT1 inhibitor RP-6306. ChemRxiv. DOI 10.26434/chemrxiv-2022-2g6m6.

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