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SIAIS178

SIAIS178 Structure
SIAIS178 structure
CAS No.
2376047-73-1
Chemical Name:
SIAIS178
Synonyms
SIAIS178;N-(2-Chloro-6-methylphenyl)-2-((6-(4-(8-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-8-oxooctanoyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide;N-(2-chloro-6-methylphenyl)-2-({6-[4-(7-{[(2S)-1-[(2S,4R)-4-hydroxy-2-({[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}carbamoyl)pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl}heptanoyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide
CBNumber:
CB68049335
Molecular Formula:
C50H62ClN11O6S2
Molecular Weight:
1012.68
MDL Number:
MFCD32689531
MOL File:
2376047-73-1.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-05-28 05:53:48
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SIAIS178 Properties

Density 1.335±0.06 g/cm3(Predicted)
pka 10.94±0.70(Predicted)
form Solid
color White to off-white

SAFETY

Risk and Safety Statements

Symbol(GHS)  Exclamation Mark (GHS07)
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319
Precautionary statements  P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

SIAIS178 price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Biosynth BVD04773 SIAIS178 2376047-73-1 1mg $359.81 2026-06-04 Buy
Biosynth BVD04773 SIAIS178 2376047-73-1 5mg $1169.4 2026-06-04 Buy
Biosynth BVD04773 SIAIS178 2376047-73-1 10mg $1870.9 2026-06-04 Buy
Biosynth BVD04773 SIAIS178 2376047-73-1 25mg $3508.25 2026-06-04 Buy
Biosynth BVD04773 SIAIS178 2376047-73-1 50mg $5613.5 2026-06-04 Buy
Product number Packaging Price Buy
BVD04773 1mg $359.81 Buy
BVD04773 5mg $1169.4 Buy
BVD04773 10mg $1870.9 Buy
BVD04773 25mg $3508.25 Buy
BVD04773 50mg $5613.5 Buy

SIAIS178 Chemical Properties, Uses, Production

Description

SIAIS178 is a potent BCR-ABL Degrader. SIAIS178 induces proper interaction between BCR-ABL and VHL ligase leading to effective degradation of BCR-ABL protein, achieves significant growth inhibition of BCR-ABL+ leukemic cells in vitro, and induces substantial tumor regression against K562 xenograft tumors in vivo. In addition, SIAIS178 also degrades several clinically relevant resistance-conferring mutations. Our data indicate that SIAIS178 as efficacious BCR-ABL degrader warrants extensive further investigation for the treatment of BCR-ABL+ leukemia.

Uses

SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity[1].

in vivo

SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement [1].
SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively[1].

Animal Model:NOD/SCID mice with termed K562-Luc[1]
Dosage:5, 15, and 45 mg/kg
Administration:Ip; 12 days
Result:Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement.
Animal Model:Female Wistar rats[1]
Dosage:2 mg/kg (Pharmacokinetic Analysis)
Administration:Iv or ip; 24 hours
Result:Had T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively.

IC 50

VHL; Bcr-Abl: 24 nM (IC50)

References

[1] Zhao Q, et al. Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. J Med Chem. 2019 Oct 24;62(20):9281-9298. DOI:10.1021/acs.jmedchem.9b01264

SIAIS178 Preparation Products And Raw materials

Raw materials

Preparation Products

SIAIS178 Suppliers

Global Suppliers ( 16)
Supplier Tel Email Country ProdList Advantage
Shanghai YuanYe Biotechnology Co., Ltd. 15026964105 2881489226@qq.com China 87240 60
Shanghai Chaolan Chemical Technology Center QQ：65489617 13301690235 Sales@ATKchemical.com China 9729 58
Jilin Province Woda Biotechnology Co., Ltd. 13504435624 1927928688@qq.com China 1644 58
TargetMol Chemicals Inc. +1-781-999-5354; +1-00000000000 marketing@targetmol.com United States 32431 58
Chengdu Peter-like Biotechnology Co., Ltd. 18108052721 2850505130@qq.com China 5037 58
ChemeGen(Shanghai) Biotechnology Co.,Ltd. 18818260767 sales@chemegen.com China 11123 58
Shanghai Maclean Biochemical Technology Co., LTD 021-50706066 15221275939 shenlinxing@macklin.cn China 29676 58
ShenZhen Trendseen Biological Technology Co.,Ltd. 13417589054 trendseenbio@gmail.com China 9067 58
Jilin Chinese Academy of Sciences-yanshen Technology 18143011203 ET-market@chemextension.com China 39244 58
Shandong Dayou Pharmaceutical Research and Development Co., Ltd. hanfangpharma@126.com 15165037910 dayouchem@126.com China 29996 58
Supplier Advantage
Shanghai YuanYe Biotechnology Co., Ltd. 60
Shanghai Chaolan Chemical Technology Center 58
Jilin Province Woda Biotechnology Co., Ltd. 58
TargetMol Chemicals Inc. 58
Chengdu Peter-like Biotechnology Co., Ltd. 58
ChemeGen(Shanghai) Biotechnology Co.,Ltd. 58
Shanghai Maclean Biochemical Technology Co., LTD 58
ShenZhen Trendseen Biological Technology Co.,Ltd. 58
Jilin Chinese Academy of Sciences-yanshen Technology 58
Shandong Dayou Pharmaceutical Research and Development Co., Ltd. 58

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SIAIS178 N-(2-chloro-6-methylphenyl)-2-({6-[4-(7-{[(2S)-1-[(2S,4R)-4-hydroxy-2-({[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}carbamoyl)pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl}heptanoyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide N-(2-Chloro-6-methylphenyl)-2-((6-(4-(8-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-8-oxooctanoyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide 2376047-73-1