BGB-15025
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 123077

CAS#: 2766481-17-6

Description: BGB-15025 is a potent and selective HPK1 inhibitor. BGB-15025 potently inhibits HPK1 kinase activity in biochemical assay, with a 50% inhibitory concentration (IC50) of 1.04 nM under Km concentration of ATP. Consistently, BGB-15025 can potently reduce SLP76 phosphorylation and increase downstream ERK phosphorylation in a concentration dependent manner in T cells-based assay. As a consequence, BGB-15025 induces TCR activation and IL-2 production in T cells.

Chemical Structure

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BGB-15025
CAS# 2766481-17-6
Instruction

Theoretical Analysis

MedKoo Cat#: 123077
Name: BGB-15025
CAS#: 2766481-17-6
Chemical Formula: C28H37FN8O2
Exact Mass: 536.30
Molecular Weight: 536.660
Elemental Analysis: C, 62.67; H, 6.95; F, 3.54; N, 20.88; O, 5.96

Price and Availability

Size Price Availability Quantity
10mg USD 450 2 Weeks
25mg USD 750 2 Weeks
50mg USD 1250 2 Weeks
100mg USD 1950 2 Weeks
1g USD 6950 2 Weeks
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Synonym: EX-A6852; BGB 15025; BGB15025; BGB-15025; 2766481-17-6;

IUPAC/Chemical Name: 4-[5-amino-6-[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]oxypyrazin-2-yl]-N-[2-[(3R)-3-fluoropyrrolidin-1-yl]ethyl]-2,6-dimethylbenzamide

InChi Key: IGTYEXMPMYGLTR-OAQYLSRUSA-N

InChi Code: InChI=1S/C28H37FN8O2/c1-18-12-20(13-19(2)25(18)27(38)31-7-11-36-10-4-21(29)16-36)24-15-32-26(30)28(34-24)39-23-14-33-37(17-23)22-5-8-35(3)9-6-22/h12-15,17,21-22H,4-11,16H2,1-3H3,(H2,30,32)(H,31,38)/t21-/m1/s1

SMILES Code: O=C(NCCN1C[C@H](F)CC1)C2=C(C)C=C(C3=NC(OC4=CN(C5CCN(C)CC5)N=C4)=C(N)N=C3)C=C2C

Appearance: To be determined

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Hematopoietic progenitor kinase 1 (HPK1), a hematopoietic cell-restricted serine/threonine protein kinase, has been reported to serve as a critical negative feedback regulator of T lymphocytes by phosphorylating the adaptor protein SLP76 in the TCR complex. The negative feedback role of HPK1 in TCR signaling makes it a promising target for immuno-oncology therapy. It has been recently demonstrated that the kinase activity of HPK1 is essential for its antitumor activity, and HPK1 inhibitors can be potentially combined with immune checkpoint inhibitor therapy (such as PD-1 antibody) for effective cancer treatment. BGB-15025 is a potent and selective HPK1 inhibitor that can be used as a single agent or in combination with PD-1 antibody in multiple tumor models. It is under development for the treatment of solid tumor, colorectal cancer, and non-small cell lung cancer

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 536.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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