XZ739

XZ739, a CRBN-dependent PROTAC BCL-XL degrader with a DC50 value of 2.5 nM in MOLT-4 cells after 16 h treatment. XZ739 also induces cell death through caspase-mediated apoptosis.

Product information

CAS Number: 2365172-19-4

Molecular Weight: 1349.99

Formula: C65H76ClF3N8O12S3

Chemical Name: 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{4-[(2R)-16-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}-5-methyl-2-[(phenylsulfanyl)methyl]-8,11,14-trioxa-1,5-diazahexadecan-1-yl]-3-trifluoromethanesulfonylbenzenesulfonyl}benzamide

Smiles: CC1(C)CC(CN2CCN(CC2)C2C=CC(=CC=2)C(=O)NS(=O)(=O)C2=CC(=C(C=C2)N[C@@H](CSC2C=CC=CC=2)CCN(C)CCOCCOCCOCCNC2=CC=CC3=C2C(=O)N(C2CCC(=O)NC2=O)C3=O)S(=O)(=O)C(F)(F)F)=C(CC1)C1C=CC(Cl)=CC=1

InChiKey: RTASGZOITGGVPZ-YJUSKGKKSA-N

InChi: InChI=1S/C65H76ClF3N8O12S3/c1-64(2)26-24-52(44-12-16-47(66)17-13-44)46(41-64)42-75-29-31-76(32-30-75)49-18-14-45(15-19-49)60(79)73-92(85,86)51-20-21-54(57(40-51)91(83,84)65(67,68)69)71-48(43-90-50-8-5-4-6-9-50)25-28-74(3)33-35-88-37-39-89-38-36-87-34-27-70-55-11-7-10-53-59(55)63(82)77(62(53)81)56-22-23-58(78)72-61(56)80/h4-21,40,48,56,70-71H,22-39,41-43H2,1-3H3,(H,73,79)(H,72,78,80)/t48-,56?/m1/s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 20 mg/mL (14.81 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

XZ739 (0.001-10 μM; 48 hours) potently reduces the viability of T-ALL MOLT-4, B-ALL RS4; 11, SCLC NCI-H146 cells, and platelets after 48 h treatment with IC50s of 10.1, 41.8, 25.3, and 1217 nM, respectively. XZ739 has >100-fold selectivity for MOLT-4 cells over human platelets. XZ739 (1.2-300 nM; 16 hours) induces BCL-XL degradation in MOLT-4 cells. The BCL-XL degradation induced by XZ739 in MOLT-4 is rapid, starting within 2 h; and 8 h after XZ739 treatment, more than 96% of the BCL-XL is degraded with 100 nM of XZ739.

Products are for research use only. Not for human use.