BBI-2779 free base · Synonyms: BBI 2779 · BBI2779

BBI-2779 is a potent, selective and orally bioavailable inhibitor of CHK1.

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

Target Checkpoint Kinase (Chk)

Research area Cancer

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Data Sheet SDS COA

BBI-2779 structure

CAS No.: 2871057-47-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 mg	USD 412.00	BP-02275-5mg	In stock	Get quote
10 mg	USD 716.00	BP-02275-10mg	In-stock	Get quote
25 mg	USD 1,088.00	BP-02275-25mg	In-stock	Get quote
100 mg	USD 3,116.00	BP-02275-100mg	In-stock	Get quote
250 mg	Inquire	BP-02275-250mg	Inquire	Inquire
500 mg	Inquire	BP-02275-500mg	Inquire	Inquire
1 g	Inquire	BP-02275-1g	Inquire	Inquire

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Description

BBI-2779 is a potent, selective and orally bioavailable inhibitor of CHK1 with biochemical IC50 of 0.5 nM and cellular IC50 of 3 nM (pCHK1-S345 activity in HT29 cells), 160-fold selective for CHK1 over CHK2.

Biological activity

In Vitro BBI-2779 selectively eliminates ecDNA-positive tumor cells by exploiting transcription-replication conflicts to induce synthetic lethality, and blocks ecDNA-mediated acquired resistance to targeted therapies in in vitro models[1]. BBI-2779 potently and selectively inhibits CHK1 in a cell-free biochemical assay with an IC50 of 0.3 nM and 160-fold selectivity over CHK2; it inhibited CHK1 activity, with an IC50 of 3 nM in HT29 cells[2]. BBI-2779 (3-12 nM; 24 h) induces dose-dependent replication stress and DNA damage, measured via pCHK1-S345, pRPA2-S8, and γH2AX expression, preferentially in ecDNA-positive COLO320DM colorectal cancer cells compared to chromosomal amplification-positive COLO320HSR cells[2]. In Vivo BBI-2779 (30 mg/kg; p.o.; every other day; 27 days) alone drives significant tumour growth inhibition in ecDNA-positive gastric cancer xenografts, and in combination with Infigratinib (HY-13311) (15 mg/kg; p.o.; once daily; 27 days) induces potent tumour regression and prevents ecDNA-mediated acquired resistance to FGFR inhibition[2].

Identifiers

SMILES: O(C1=C(C(OC)=CC=C1)C2=CC(NC=3C=NC(C#N)=CN3)=NN2)[C@H]4[C@H](N)CC4
InChIKey: LCICGMODJWMTPT-TZMCWYRMSA-N

Specifications

MW (average): 377.3999
Formula: C₁₉H₁₉N₇O₂
CAS No.: 2871057-47-3
Physical state: Solid
Color: White to off-white
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 4℃, sealed storage, 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Zhu X, Qian Y, Tang Q, Li J, Geng Y, Gong S, Jin C. Research Advances of Extrachromosomal Circular DNA in Breast Cancer. Cancer Med. 2025 Oct;14(19):e71285. doi: 10.1002/cam4.71285. PMID: 41051137; PMCID: PMC12498277.

[2]. Tang J, Weiser NE, Wang G, Chowdhry S, Curtis EJ, Zhao Y, Wong IT, Marinov GK, Li R, Hanoian P, Tse E, Mojica SG, Hansen R, Plum J, Steffy A, Milutinovic S, Meyer ST, Luebeck J, Wang Y, Zhang S, Altemose N, Curtis C, Greenleaf WJ, Bafna V, Benkovic SJ, Pinkerton AB, Kasibhatla S, Hassig CA, Mischel PS, Chang HY. Enhancing transcription-replication conflict targets ecDNA-positive cancers. Nature. 2024 Nov;635(8037):210-218. doi: 10.1038/s41586-024-07802-5. Epub 2024 Nov 6. PMID: 39506153; PMCID: PMC11540844.

[3]. Anthony B. Pinkerton, et al. Checkpoint kinase 1 (chk1) inhibitors and uses thereof. WO2022251502A1.

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