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923564-51-6 (Navitoclax)

1

Identification

Navitoclax Navitoclax
Name Navitoclax
Formula C47H55ClF3N5O6S3
MW 974.61
CAS No. 923564-51-6
EINECS
Smiles O=S(C1=CC(S(NC(C2=CC=C(N3CCN(CC4=C(CCC(C)(C4)C)C5=CC=C(Cl)C=C5)CC3)C=C2)=O)(=O)=O)=CC=C1N[[email protected]](CCN6CCOCC6)CSC7=CC=CC=C7)(C(F)(F)F)=O
Synonyms ABT-263;ABT 263;ABT263; (R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide
InChI InChI=1S/C47H55ClF3N5O6S3/c1-46(2)20-18-42(34-8-12-37(48)13-9-34)36(31-46)32-55-22-24-56(25-23-55)39-14-10-35(11-15-39)45(57)53-65(60,61)41-16-17-43(44(30-41)64(58,59)47(49,50)51)52-38(19-21-54-26-28-62-29-27-54)33-63-40-6-4-3-5-7-40/h3-17,30,38,52H,18-29,31-33H2,1-2H3,(H,53,57)/t38-/m1/s1
2

Introduction

ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM. IC50 Value: ≤ 0.5 nM(Ki for Bcl-xL); ≤1 nM(Ki for Bcl-2); ≤1 nM(Ki for Bcl-w) Target: Bcl-2 Family in vitro: ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively.

Background Information

A potent selective and orally bioavailable inhibitor of B-cell lymphoma-2 (BCL-2) family proteins ......by AOBIOUS INC
Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds with high affinity (Ki < 1 nM) to multiple anti-apoptotic Bcl-2 family proteins including Bcl-xL, Bcl-2 and Bcl-w. ......by MedChemexpress Co., Ltd.
Shelf life: >2 years if stored properly Drug formulation: ......by MedKoo Biosciences, Inc.
ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2. ......by Selleck Chemicals LLC
ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Cell lines SCLC cell lines
Conditions 0-1 μM; 48 hours
Method Human tumor cell lines SCLC cell lines are maintained at 37 °C containing 5% CO2. SCLC cell lines are cultured in RPMI 1640 with 10% fetal bovine serum (FBS), 1% sodium pyruvate, 25 mM HEPES, 4.5 g/L glucose, and 1% penicillin/streptomycin. Leukemia and lymphoma cell lines are cultured in RPMI 1640 supplemented with 10% FBS and 1% penicillin/streptomycin. Cells (1-5×10 4) are treated by ABT-263 for 48 hours in 96-well culture plates in a final volume of 100 μL and cytotoxicity is assessed with the CellTiter Glo assay. In vitro cyto toxicity of ABT-263 is assayed.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models C.B.-17 scid-bg or C.B.-17 scid mice
Dosage 100 mg/kg/d
Formulation Formulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG
Administration Administered via p.o.
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000029152

Storage condition

Solubility

DMSO ≥190mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 100 mg/mL (102.6 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM) by Selleck Chemicals LLC
5

Mechanism and Indication

Signaling Pathways Apoptosis
Target Bcl-2 Family
Research Area Cancer
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Navitoclax - Phase 2 Clinical
Navitoclax - Phase 2
7

Safety Data of Navitoclax

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD18() USA
Active Biopharma Corp China
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD50();10mg/USD70() USA
MedChemexpress Co., Ltd. 5mg/USD50();10mg/USD70() USA
MedKoo Biosciences, Inc. USA
Rosewell Industry Co., Ltd. China
Selleck Chemicals LLC 5mg/USD120(In stock);10mg/USD200(In stock);25mg/USD370(In stock);10mM/1mLIn DMSO/USD400(In stock);100mg/USD970(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD50();10mg/USD70() China
Target Molecule Corp. 5mg/USD102();10mg/USD188();50mg/USD324() USA
10

Related Products

Other Forms of 923564-51-6

Name CAS No Formula MW
GCN2-IN-3 1448694-02-7 C23H29N9O 447.54
GCN2-IN-2 1448693-80-8 C19H18ClFN8O 428.85
GCN2-IN-1 1448693-69-3 C19H18N10O 402.41
GGTI298 180977-44-0 C27H33N3O3S 479.63
Bisantrene 78186-34-2 C22H22N8 398.46
PF-1355 1435467-38-1 C14H15N3O4S 321.35
KRIBB11 342639-96-7 C13H12N6O2 284.27
WT-161 1206731-57-8 C27H30N4O3 458.55
ABX464 1258453-75-6 C16H10ClF3N2O 338.71

Recommended Compounds in Bcl-2 Family

Name CAS No Formula MW
MIM1 509102-00-5 C17H21N3O3S 347.43
713492-66-1
Gossypol (acetic acid) 12542-36-8 C32H34O10 578.6064
Marinopyrrole A 1227962-62-0 C22H12Cl4N2O4 510.15
WEHI-539 1431866-33-9 C31H29N5O3S2 583.72
Gambogic Acid 2752-65-0 C38H44O8 628.75
ABT-199 1257044-40-8 C45H50ClN7O7S 868.44
(±)-Apogossypol 475-56-9 C28H30O6 462.5342
Gossypol 303-45-7 C30H30O8 518.55
AT-101 90141-22-3 C30H30O8 518.55
BAM7 331244-89-4 C21H19N5O2S 405.47
SZ4TA2 406231-90-1 C28H32N4O5S2 568.71
TW-37 877877-35-5 C33H35NO6S 573.7
HA14-1 65673-63-4 C17H17BrN2O5 409.23
Obatoclax 803712-79-0 C21H23N3O4S 413.49
ABT-737 852808-04-9 C42H45ClN6O5S2 813.43
Bax inhibitor peptide V5 579492-81-2 C27H50N6O6S 586.79
A-1331852 1430844-80-6 C38H38N6O3S 658.81
A-1155463 1235034-55-5 C35H32FN5O4S2 669.79
Bz 423 216691-95-1 C27H21ClN2O2 440.92

Recommended Compounds in Same Indication

Name CAS No Formula MW
11

Route of Synthesis

12

References

[1]. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program Pediatric Blood & Cancer 50, Pages 1181 – 1189

[2]. Wong M, Tan N, Zha J, Peale FV, Yue P, Fairbrother WJ, Belmont LD.Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models.Mol Cancer Ther. 2012 Apr;11(4):1026-35. Epub 2012 Feb 1.

[3]. Rudin CM, Hann CL, Garon EB, Ribeiro de Oliveira M, Bonomi PD, Camidge DR, Chu Q, Giaccone G, Khaira D, Ramalingam SS, Ranson MR, Dive C, McKeegan EM, Chyla BJ, Dowell BL, Chakravartty A, Nolan CE, Rudersdorf N, Busman TA, Mabry MH, Krivoshik AP, Humerickhouse RA, Shapiro GI, Gandhi L.Phase II study of single-agent navitoclax (ABT-263) and biomarker correlates in patients with relapsed small cell lung cancer.Clin Cancer Res. 2012 Jun 1;18(11):3163-9. Epub 2012 Apr 11.

[4]. Ackler S, Mitten MJ, Chen J, Clarin J, Foster K, Jin S, Phillips DC, Schlessinger S, Wang B, Leverson JD, Boghaert ER.Navitoclax (ABT 263) and Bendamustine ± Rituximab Induce Enhanced Killing of Non-Hodgkin's Lymphoma Tumors in Vivo.Br J Pharmacol. 2012 May 24.

[5]. Mérino D, Khaw SL, Glaser SP, Anderson DJ, Belmont LD, Wong C, Yue P, Robati M, Phipson B, Fairlie WD, Lee EF, Campbell KJ, Vandenberg CJ, Cory S, Roberts AW, Ludlam MJ, Huang DC, Bouillet P.Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells.Blood. 2012 Jun 14;119(24):5807-16. Epub 2012 Apr 26.

Protocol Reference

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More Information

Navitoclax

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