Table 1. Summary of SU5416 and SU6668... | American Society of Hematology

Table 1.

Summary of SU5416 and SU6668 activity in patient blast samples

Patient no.	Diagnosis	Cytogenetics	% Blasts	% c-kit	c-kit positivity inhibition		Apoptosis
Patient no.	Diagnosis	Cytogenetics	% Blasts	% c-kit	SU5416	SU6668	SU5416	SU6668
1	AML relapsed	Trisomy 4, trisomy 21, trisomy 22	90	80	+^*	+	+^1-153	NT
2	AML refractory	t(1;2), -5, del(6), del(8), del(13), del(17), del(18), del(21)	60	50	+	NT	+^1-153	NT
3	Myelodysplastic syndrome, T-ALL	t(5;13), t(22;21)	87	19	+	NT	+	NT
4	CML Blast crisis	t(9;22)	31	13	NT	NT	+^‡,^1-155	+^‡,^1-155
5	AML relapsed	−16, t(1;21) Trisomy 21	94	12	NT	NT	NT	+^‡
6	AML newly diagnosed	t(3;9), t(8;21)	23	43	NT	NT	+^1-155	NT
7	AML refractory	−5, −6	36	47	NT	NT	+	+
8	AML relapsed	Trisomy 8, trisomy 13	97	40	+^†	+	+^‡,^1-153	+^‡,^1-153
9	AML refractory	Not determined	75	81	NT	NT	+^1-155	NT

Patient no.	Diagnosis	Cytogenetics	% Blasts	% c-kit	c-kit positivity inhibition		Apoptosis
Patient no.	Diagnosis	Cytogenetics	% Blasts	% c-kit	SU5416	SU6668	SU5416	SU6668
1	AML relapsed	Trisomy 4, trisomy 21, trisomy 22	90	80	+^*	+	+^1-153	NT
2	AML refractory	t(1;2), -5, del(6), del(8), del(13), del(17), del(18), del(21)	60	50	+	NT	+^1-153	NT
3	Myelodysplastic syndrome, T-ALL	t(5;13), t(22;21)	87	19	+	NT	+	NT
4	CML Blast crisis	t(9;22)	31	13	NT	NT	+^‡,^1-155	+^‡,^1-155
5	AML relapsed	−16, t(1;21) Trisomy 21	94	12	NT	NT	NT	+^‡
6	AML newly diagnosed	t(3;9), t(8;21)	23	43	NT	NT	+^1-155	NT
7	AML refractory	−5, −6	36	47	NT	NT	+	+
8	AML relapsed	Trisomy 8, trisomy 13	97	40	+^†	+	+^‡,^1-153	+^‡,^1-153
9	AML refractory	Not determined	75	81	NT	NT	+^1-155	NT

Blasts were isolated from peripheral blood samples from patients with the indicated diagnoses; % blasts and % c-kit positivity are indicated. For phosphorylation assays, SU5416 was used at 5 μM, except where indicated, and SU6668 was tested at 0.5 and 5 μM. Apoptosis was assessed by flow cytometric analysis of activated caspase-3 except where indicated. Apoptosis assays were done with 25 μM SU5416 or SU6668 except where indicated.

+ indicates that inhibition of phosphorylation or induction of apoptosis was observed.

NT indicates the sample was not tested, due to limiting cell number.

SU5416 was tested at 0.05, 0.5, and 5 μM.

†

SU5416 was tested at 0.5 and 5 μM.

‡

Compounds were tested at 5 and 25 μM.

F1-153

Apoptosis was assessed using assays measuring caspase-3 activation and PARP cleavage.

F1-155

Apoptosis was assessed with PARP cleavage assay only.

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