A PROTAC that drives Bcr-Abl degradation
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GMB 475

Item No. 40463

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(4R)-3-methyl-N-[2-[2-[4-[6-[[4-(trifluoromethoxy)phenyl]amino]-4-pyrimidinyl]phenoxy]ethoxy]acetyl]-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-L-prolinamide
CAS Number
2490599-18-1
Molecular Formula
C43H46F3N7O7S
Formula Weight
861.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C(N(C[C@@H]1O)[C@@H](C1)C(NCC2=CC=C(C(SC=N3)=C3C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCOC4=CC=C(C5=NC=NC(NC(C=C6)=CC=C6OC(F)(F)F)=C5)C=C4)=O
InChi Code
InChI=1S/C43H46F3N7O7S/c1-26-38(61-25-50-26)29-7-5-27(6-8-29)21-47-40(56)35-19-31(54)22-53(35)41(57)39(42(2,3)4)52-37(55)23-58-17-18-59-32-13-9-28(10-14-32)34-20-36(49-24-48-34)51-30-11-15-33(16-12-30)60-43(44,45)46/h5-16,20,24-25,31,35,39,54H,17-19,21-23H2,1-4H3,(H,47,56)(H,52,55)(H,48,49,51)/t31-,35+,39-/m1/s1
InChi Key
ONDVWISBMHHLGZ-SBJIGXGQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $82

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    10 mg

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    25 mg

    $367

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    50 mg

    $611

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    Product Description

    GMB 475 is a proteolysis-targeting chimera (PROTAC) containing the Bcr-Abl inhibitor GNF-5 (Item No. 16254) conjugated to VHL ligand 1 (Item No. 21591).1 It induces degradation of Bcr-Abl with a half-maximal degradation concentration (DC50) value of 340 nM. GMB 475 selectively inhibits the proliferation of K562 chronic myeloid leukemia (CML) and Bcr-Abl-expressing Ba/F3 cells (IC50 = ~1 µM for both) over parental Ba/F3 cells (IC50 = >10 µM). It also inhibits the proliferation of Ba/F3 cells expressing mutant Bcr-Abl (IC50s = 1.98 and 0.37 µM for Bcr-AblT315I and Bcr-AblG250E, respectively). GMB 475 (2.5 µM) induces apoptosis in primary human CML cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burslem, G.M., Schultz, A.R., Bondeson, D.P., et al. Targeting BCR-ABL1 in chronic myeloid leukemia by PROTAC-mediated targeted protein degradation. Cancer Res. 79(18), 4744-4753 (2019).