PTC596 free base · Synonyms: Unesbulin

PTC596 is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 inhibitor.

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

Target BMI1 Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

PTC596 structure

CAS No.: 1610964-64-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 480.00	BP-01904-100mg	In stock	Get quote
250 mg	USD 920.00	BP-01904-250mg	In stock	Get quote
500 mg	USD 1,420.00	BP-01904-500mg	In stock	Get quote
1 g	USD 2,120.00	BP-01904-1g	In stock	Get quote
5 g	Inquire	BP-01904-5g	Inquire	Inquire

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Description

PTC596 is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. PTC596 targets BMI1 expressed by both tumor cells and cancer stem cells (CSCs), and induces hyper-phosphorylation of BMI1, leading to its degradation.

Biological activity

In Vitro Unesbulin (PTC596; 20-200 nM; for 48 hours) induces apoptosis in AML cells in a p53-independent manner. BMI-1 overexpression desensitizes AML cells to PTC596-induced apoptosis. Unesbulin (200 nM; for 10 hours) leads to an accumulation of cells in G2/M phase. Unesbulin (0.012-1 μM; for 20 hours) significantly reduces protein levels of BMI-1. Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1. In Vivo Unesbulin (PTC596; 5 mg/kg; oral gavage; every 3 days for 13 days) significantly prolongs mouse survival. Unesbulin (20 mg/kg; oral gavage; once a week for 15 days) causes tumor volume significantly smaller than that of control SCID mice with K562 cells. Unesbulin (10 or 12.5 mg/kg; oral gavage; twice a week until death) causes the survival significantly longer than the vehicle-treated group in NOD-SCID mice with HL-60 cells.

Identifiers

SMILES: NC1=C(F)C(NC2=CC=C(C(F)(F)F)C=C2)=NC(N3C4=CC(F)=CC=C4N=C3C)=N1
InChIKey: TWLWOOPCEXYVBE-UHFFFAOYSA-N

Specifications

MW (average): 420.3387
Formula: C₁₉H₁₃F₅N₆
CAS No.: 1610964-64-1
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 -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Nishida Y, et al. The novel BMI-1 inhibitor PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells. Blood Cancer J. 2017 Feb 17;7(2):e527.

[2]. BMI1 inhibitor PTC596

Same target

Search BMI1

Same research area

Search Cancer