DCC-2036 (Rebastinib)|2mg|K1328-上海高创化学科技有限公司

DCC-2036 (Rebastinib)

报价：¥1298

供货周期：

7天

品牌：

型号：

2mg

货号：

K1328

CAS号：

1020172-07-9

SKU:K1328		M. Wt:553.59
Formula:C30H28FN7O3		Solubility:No
Purity:>99%		Storage:2 years at -20 degrees centigrade
CAS No.:1020172-07-9		Synonyms:N/A
Chemical NameN/A

Description	DCC-2036 (Rebastinib)
Targets
IC50	N/A
In vitro	The lead "switch-control" inhibitor, DCC-2036, can potently inhibit autophosphorylation of ABL and ABL(T315I) enzymes with IC50 of 0.8 nM and 4 nM. DCC-2036 inhibitS Ba/F3 cells expressing BCR-ABL and BCR-ABL(T315I) with IC50 of 19 nM and 63 nM. Ex vivo exposure of CML cells from patients harboring BCR-ABL or BCR-ABL(T315I) to DCC-2036 reveals marked inhibition of colony formation and reduces phosphorylation of the direct BCR-ABL target CrkL. DCC-2036 potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant CML-resistance mutants, including T315I.
In vivo	DCC-2036 inhibits BCR-ABL1(T315I)-expressing cell lines, prolongs survival in mouse models of T315I mutant CML and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing T315I in vitro and in vivo, supporting its clinical development in TKI-resistant Ph(+) leukemia.
Clinical Trials	N/A
Features	N/A

Description

DCC-2036 (Rebastinib)

Targets

IC50

N/A

In vitro

The lead "switch-control" inhibitor, DCC-2036, can potently inhibit autophosphorylation of ABL and ABL(T315I) enzymes with IC50 of 0.8 nM and 4 nM. DCC-2036 inhibitS Ba/F3 cells expressing BCR-ABL and BCR-ABL(T315I) with IC50 of 19 nM and 63 nM. Ex vivo exposure of CML cells from patients harboring BCR-ABL or BCR-ABL(T315I) to DCC-2036 reveals marked inhibition of colony formation and reduces phosphorylation of the direct BCR-ABL target CrkL. DCC-2036 potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant CML-resistance mutants, including T315I.

In vivo

DCC-2036 inhibits BCR-ABL1(T315I)-expressing cell lines, prolongs survival in mouse models of T315I mutant CML and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing T315I in vitro and in vivo, supporting its clinical development in TKI-resistant Ph(+) leukemia.

Clinical Trials

N/A

Features

N/A