MK-1775 free base · Synonyms: Adavosertib

Adavosertib is a potent and selective Wee1 inhibitor.

For research use only. Not for human or veterinary use.

Target Wee1

Research area Cancer

Purity >=99.5% Stock Inquire

Data Sheet SDS COA

MK-1775 structure

CAS No.: 955365-80-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
2 g	USD 448.00	BP-02302-2g	In stock	Get quote
3 g	USD 537.00	BP-02302-3g	In stock	Get quote
5 g	USD 716.00	BP-02302-5g	In stock	Get quote
10 g	USD 1,140.00	BP-02302-10g	In stock	Get quote
25 g	USD 2,290.00	BP-02302-25g	In stock	Get quote

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Description

Adavosertib (MK-1775, AZD1775) is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM in a cell-free assay; hinders G2 DNA damage checkpoint.

Biological activity

In Vitro Adavosertib (MK-1775) enhances the cytotoxic effects of 5-FU in p53-deficient human colon cancer cells. Adavosertib (MK-1775) inhibits CDC2 Y15 phosphorylation in cells, abrogates DNA damaged checkpoints induced by 5-FU treatment, and causes premature entry of mitosis determined by induction of Histone H3 phosphorylation. Adavosertib (MK-1775) abrogates the radiation-induced G2 block in p53-defective cells but not in p53 wild-type lines. The combination of NSC 613327 with Adavosertib (MK-1775) produces robust anti-tumor activity and remarkably enhances tumor regression response (4.01 fold) compared to NSC 613327 treatment in p53-deficient tumors. In Vivo In vivo, Adavosertib (MK-1775) potentiates the anti-tumor efficacy of 5-FU at tolerable doses. Adavosertib (MK-1775) (60 mg/kg twice daily, p.o.) enhances H1299 xenograft tumor response to fractionated radiotherapy. Adavosertib (MK-1775) (30 mg/kg. p.o.) regresses tumor growth in PANC198, PANC215 and PANC185 as compared to GEM treated mice.

Identifiers

SMILES: CN1CCN(CC1)C1=CC=C(NC2=NC=C3C(=O)N(CC=C)N(C3=N2)C2=NC(=CC=C2)C(C)(C)O)C=C1
InChIKey: BKWJAKQVGHWELA-UHFFFAOYSA-N

Specifications

MW (average): 500.5954
Formula: C₂₇H₃₂N₈O₂
CAS No.: 955365-80-7
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Hirai H, et al. Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents. Mol Cancer Ther, 2009, 8(11), 2992-3000.

Same target

Search Wee1

Same research area

Search Cancer