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BETd-246

Product Name
BETd-246
CAS No.
2140289-17-2
Chemical Name
BETd-246
Synonyms
BETd-246;BETd-246 (BETd 246;4-[(3-Cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[3-[2-[2-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]propoxy]ethoxy]ethoxy]propyl]-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide;9H-Pyrimido[4,5-b]indole-2-carboxamide, 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[3-[2-[2-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]propoxy]ethoxy]ethoxy]propyl]-6-methoxy-;4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N-(3-{2-[2-(3-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}propoxy)ethoxy]ethoxy}propyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide
CBNumber
CB84718705
Molecular Formula
C48H55N11O10
Formula Weight
946.02
MOL File
2140289-17-2.mol
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BETd-246 Property

Density 
1.51±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C, stored under nitrogen
solubility 
DMSO : 200 mg/mL (211.41 mM; Need ultrasonic)
form 
Solid
pka
10.75±0.40(Predicted)
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0087862
Product name
BETd-246
Purity
98.03%
Packaging
5mg
Price
$650
Updated
2021/12/16
ChemScene
Product number
CS-0087862
Product name
BETd-246
Purity
98.03%
Packaging
10mg
Price
$950
Updated
2021/12/16
ChemScene
Product number
CS-0087862
Product name
BETd-246
Purity
98.03%
Packaging
25mg
Price
$1950
Updated
2021/12/16
ChemScene
Product number
CS-0087862
Product name
BETd-246
Purity
98.03%
Packaging
50mg
Price
$2950
Updated
2021/12/16
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BETd-246 Chemical Properties,Usage,Production

Uses

BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity[1].

in vivo

BETd-246 (5 mg/kg, IV, 3 times per week for 3 weeks) treatment effectively inhibits WHIM24 tumor growth, similar to the antitumor activity of BETi-211 with higher dosage and more frequently administration. The treatment of 10 mg/kg induces partial tumor regression during treatment without apparent toxicity. BETd-246 has very limited drug exposure in the xenograft tumor tissue in MDA-M-231and MDA-MB-468 models[1].

Animal Model:“Washington Human in Mouse (WHIM)” (PDX) model developed from a patient with treatment-resistant breast cancer (ESRE380Q, PR- and HER2-))[1].
Dosage:5, 10 mg/kg
Administration:IV, 3 times per week for 3 weeks.
Result:Effectively inhibited WHIM24 tumor growth.

References

[1] Bai L, et al. Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer. Cancer Res. 2017 May 1;77(9):2476-2487. DOI:10.1158/0008-5472.CAN-16-2622

BETd-246 Preparation Products And Raw materials

Raw materials

Preparation Products

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BETd-246 Suppliers

Sichuan Wei Keqi Biological Technology Co., Ltd.
Tel
028-81700200 18116577057
Fax
028-81705658
Email
3003855609@qq.com
Country
China
ProdList
7778
Advantage
56
Beijing Jin Ming Biotechnology Co., Ltd.
Tel
010-60605840 18892239720
Fax
010-60605840
Email
psaitong@jm-bio.com
Country
China
ProdList
12306
Advantage
58
Shanghai finete Pharmaceutical Co., Ltd.
Tel
021-021-00000000 18221039705
Fax
QQ:17263424
Email
finetechpharm@126.com
Country
China
ProdList
214
Advantage
58
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9729
Advantage
58
Jilin Province Woda Biotechnology Co., Ltd.
Tel
13504435624
Email
1927928688@qq.com
Country
China
ProdList
1623
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32470
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Wuhan Fortuna Chemical Co., Ltd
Tel
+86-027-59207850 +86-13986145403;
Fax
86-27-59524646
Email
info@fortunachem.com
Country
China
ProdList
6011
Advantage
58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
ProdList
11218
Advantage
58
ShenZhen Trendseen Biological Technology Co.,Ltd.
Tel
13417589054
Email
trendseenbio@gmail.com
Country
China
ProdList
9069
Advantage
58
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View Lastest Price from BETd-246 manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
BETd-246 2140289-17-2
Price
US $0.00/mg
Min. Order
1mg
Purity
98%min
Supply Ability
50mg
Release date
2021-08-26

2140289-17-2, BETd-246Related Search:


  • BETd-246
  • BETd-246 (BETd 246
  • 9H-Pyrimido[4,5-b]indole-2-carboxamide, 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[3-[2-[2-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]propoxy]ethoxy]ethoxy]propyl]-6-methoxy-
  • 4-[(3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-N-(3-{2-[2-(3-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}propoxy)ethoxy]ethoxy}propyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide
  • 4-[(3-Cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino]-7-(3,5-dimethyl-4-isoxazolyl)-N-[3-[2-[2-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]propoxy]ethoxy]ethoxy]propyl]-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide
  • 2140289-17-2
  • C48H55N11O10